Phd in PHARMACEUTICAL SCIENCES

email: roberto.disanto@uniroma1.it
phone: 23150
building: CU019
room: 203

Curriculum Vitae

Roberto Di Santo
Born in Rome; 7th June 1963

Education and Training
1984−1986: undergraduate student – Department of Pharmaceutical Studies, University of Rome La Sapienza
1986: Chemistry degree: 110/110 cum laude. The thesis work was carried out under the supervision of Prof. Marino Artico. Thesis title: Synthesis of new tryciclic system 1-phenyl-1H-pyrazolo[3,4-e]indolizine and derivatives as potential aniblastic agents.
1989: Pasteur Institute – Fondazione Cenci Bolognetti fellowship
1994: Pharmacy degree: 110/110 cum laude. The thesis work was carried out under the supervision of Prof. Silvio Massa. Thesis title: Synthesi of biologically active azoles via TosMIC reaction.

Employment and Research Experience
1987-1988: Chemist Official in Italian army;
199o: assistant in Department of Studi Farmaceutici;
1996−1998: University researcher in Medicinal Chemistry at the Department of Pharmaceutical Studies University of Rome “La Sapienza”.
1998-2016: Associate professor of Medicinal Chemistry at the Department of Pharmaceutical Studies and then Chemistry and Technology of Drug, University of Rome “La Sapienza” (Scientific sector CHIM/08-Medicinal Chemistry).
2005-2012 Chairman of Class Council 24S (Degrees: ISF, Science e Technologies of Herboristical Products, and Environmental Toxicology).
2016-present: Full professor of Medicinal Chemistry at the Chemistry and Technology of Drug, University of Rome “La Sapienza” (Scientific sector CHIM/08-Medicinal Chemistry).
Teaching Medicinal Chemistry (School of Pharmacy) as regular professor: Chimica Farmaceutica e Tossicologica II (School of Pharmacy); other teaching courses: Chimica Farmaceutica e Tossicologica II (Science e Technologies of Herboristical Products); Analisi dei Medicinali I (School of Pharmacy); Analisi dei farmaci e dei loro metaboliti nei fluidi biologici (Medicinal Chemistry and Technologies).

MAIN RESEARCH INTERESTS DURING THE LAST TEN YEARS:
The research activity is focused on Drug Design and Development (DDD) of
novel drugs and performed by the means of the most modern technics in the
medicinal chemistry field like, computer driven drug design (CDDD), classical
organic synthesis, parallel synthesis, microwave applications and flow
chemistry.
The main research field are focused on chemotherapy, in particular on antiviral
(HIV, HCV, poliovirus et al.), antiprotozoal, antibacterial, and antimicobacterial
and antifungal agents, as well as on anticancer drugs.
Collaborations with companies gave results in the Alzheimer field, 5-HT4
ligands, antimalarial drugs, antitumor drugs, including anti-metastatic drug and
compounds interfering with the autophagy process.
In summary the expertise can be listed as follows in the field of:
1-Chemotheapeutic agents:
a) Antiviral compounds (HIV, HCV, Chicungunya, poliovirus, fluvirus)
b) Antifungal agents
c) Antiprotozoal agents
d) Antimiycobacterial agents
e) Antibacterial agents (resistance)
2- Antitumor agents (specific targets for personalized medicine)
3- Anti-Alzheimer
4- Ligands of 5-HT4R
More than 170 papers and 6 patents, and oral communications, in national and
international meetings.

GRANTS ACTIVE AFTER 2000 (year-grant agency-title-role)
- PNRR PE13 Spoke 5: One Health Basic and Translational Research Actions
addressing Unmet Needs on Emerging Infectious Diseases (2022-25)
- Institut Pasteur International Network: Drug Design SARS2 (2020-22)
- FP7 European Project.: Combined Highly Active Anti-retroviral Microbicides
(CHAARM) FP7 (2010-15).
- National Coordinator National Research Project 2010 (PRIN) anti-HIV agents.
- National Coordinator National Research Project 2008 (PRIN) anti-HIV agents
targeting innovative viral and human targets.
- National Coordinator National Research Project 2006 (PRIN) anti-HIV agents
acting on novel targets.
- National Program against AIDS 2009: New quinolones acting as microbicides.
- VI National Program against AIDS: Synthesis enzyme assays and antiviral
activity of novel HIV integrase inhibitors.
- V National Program against AIDS: Novel HIV integrase inhibitors.
- PI for Department of Pharmaceutical Studies of joint project ISS-NIH on HIV
integrase inhibitors.
- PI Bill e Melinda Gates Foundation - CPDD Grant 2009 – Protein
farnesyltransferase inhibitors as anti-HAT agents and anti-Leishmanial
compounds.
- PI Pasteur Institute- Fondazione Cenci Bolognetti - Grant 2008-10 –
Inhibitors of RNase H function of the HIV reverse transcriptase.
- PI Pasteur Institute- Fondazione Cenci Bolognetti - Grant 2011-13 – New
azole derivative sas antiprotozoal agents.
- PI Pasteur Institute- Fondazione Cenci Bolognetti - Grant 2014-16 – Dual
integrase and RNase H inhibitors to defeat HIV.
- PI Pasteur Institute- Fondazione Cenci Bolognetti - Grant 2020-22 –
Targeting Trypanosomatids sterol biosynthesis and thiol redox metabolism
key enzymes for lead drug discovery.
- Joint research with Sigma-Tau Company - Grant 1999-2011 – Beta-amiloid
project.
- Joint research with Sigma-Tau Company - Grant 2004-2010 – Malaria
Artekin.
- Joint research with Sigma-Tau Company - Grant 2018-2019 – Triamcinolone
- Joint research with Sigma-Tau Company - Grant 2021-2022 – Brilacidin
- Joint research with ACRAF Company - Grant 2003-2008 – Ligands of 5-HT4
receptor.
- Joint research with Sigma-Tau Company - Grant 2013-2016 – Small
molecules as inhibitors of heparanase.
- Participant of several National Project (PRIN) 1997, 2000, 2001, 2002 and
FIRB 2002

International collaborations:
- D. Rauh, Max-Plank Institut, Dortmund University (Germany)
- L. Podust, UCSan Diego, San Diego (USA)
- F. Agou, Pasteur Institu Paris, Paris (France)
- Y. Pommier, NHI, National Cancer Institute, Bethesda (USA)
- S. J. Le Grice, NHI, National Cancer Institute, Frederick (USA)
- H. Waldmann, Max-Plank Institut, Dortmund University (Germany)
- Michael Gelb, Washington University, Seattle (USA)
- Z. Debyser Catholic University of Leuven (KUL) (Belgium)
- G. Vanham Antwerpen University (Belgium)
- K. Augustyns Antwerpen University (Belgium)
- M. Delarue Pasteur Istitut of Paris (France)
- R. Brosch Pasteur Istitut of Paris (France)
- R. Brunn Swiss Tropical Institute Parasite Chemotherapy Basilea (Swissland)
- L. Maes Antwerpen University (Belgium)
- A. Siddiqui, University of Colorado (USA)
- I. Sattler, Hans-Knoell Institut, Jena (Germany)
- S. Rault, CERMN, University of Caen (France),
- S. B. Jensen PET-center Århus University Hospital Århus C (Denmark)


ADDITIONAL INFORMATION

BIBLIOMETRIC DATA: 170 papers in international refereed journals. Six patents.
h-index 34, citations > 3800 (data from Scopus).
h-index 40, citations > 5000 (data from Scholar)
Advisory bord for a few of journals in the field of medicinal chemistry.
Referee for scientific publications: Journal of Medicinal Chemistry, Bioorganic and Medicinal Chemistry, Bioorganic and Medicinal ChemistryLetters, Current Medicinal Chemistry, ChemMedChem, Journal of Heterocyclic Chemistry.

Referee for national and international granting agencies.
He has participated as an invited speaker to several international congresses of the Medicinal Chemistry area.

Scientific Appointments
Member of European Federation of Medicinal Chemistry (EFMC)
2024 Chairman of the International Symposium on Medicinal Chemistry – EFMC, Rome 2024.
2022 – 2024 International Organizing Committee International Symposium on Medicinal
Chemistry – EFMC, Rome 2024.
2020 – 2022 International Organizing Committee International Symposium on Medicinal
Chemistry – EFMC, Nice 2022.
2016 – 2018 International Organizing Committee International Symposium on Medicinal
Chemistry – EFMC, Lubiana 2018.
2014 “Biotech, SME, pharma landscape and how to interact with that landscape” EFMC
working group.
Member of Italian Chemical Society (SCI), Division of Medicinal Chemistry.
2019-2021 Executive Committee of Division of Medicinal Chemistry of SCI.
2019-2021 Vice President of Division of Medicinal Chemistry of SCI.
2016-2018 Executive Committee of Division of Medicinal Chemistry of SCI.
2016-2018 Treasurer of Division of Medicinal Chemistry of SCI.
Scientific Committee XXII National Meeting on Medicinal Chemistry – Rome 2013
Organizing Committee XXII National Meeting on Medicinal Chemistry – Roma 2013
Member of Scientific Committee of “Laboratory of Synthetic Methodologies in Medicinal
Chemistry”, University of Siena.

Patents

1) R. Di Santo, Y. Pommier, C. Marchand, M. Artico, R. Costi.
Preparation of quinolin-4-ones as inhibitors of retroviral integrase for the treatment of HIV, AIDS and aids related complex (ARC).
PCT Int. Appl. (2005), 75 pp. WO 2005087759 A1 20050922 CAN 143:326228 AN 2005:1026945.
2) P. Minetti, R. Di Santo.
Naphthyl derivatives inhibitors of the beta-amyloid aggregation.
EP 05022706.5; 518/EP, 18 october 2005.
3) M. A. Alisi, N. Cazzolla, R. Costi, R. Di Santo, G. Furlotti, A. Guglielmotti, L. Polenzani.
Pyrroloquinolines with serotoninergic activity, process for preparing it and pharmaceutical composition comprising it.
PCT/EP2009/059216, WO 2010012611, CAN 152:238937
4) P. Valenti, T. Natalizi, R. Di Santo, L. Pescatori, G. Cuzzucoli Crucitti, A. Ilari, E. Chiancone.
Pyrrolyl-hydroxamates for use in the prevention and/or treatment of bacterial infections
PCT Int. Appl. (2013), WO 2013182254 A1 20131212.
5) G. Giannini, G. Battistuzzi, R. Di Santo, R. Costi, A. Messore “Symmetrical 2-aminophenyl-benzazolyl-5-acetate compounds and their use as anti-heparanase” EP17163014.8, 27.03.2017, WO 2018/177857 A1 04/10/2018
6) G. Giannini, G. Battistuzzi, R. Di Santo, R. Costi, V. N. Madia 2-(4-(4-(Bromomethoxybenzamido)benzylamino)phenyl)benzazole derivatives and their use as anti-heparanase EP17163015.5, 27.03.2017, WO 2018/177860 A1 04/10/2018

____________________________________________________________________
Personal bibliography (2012-today)

1) G. Cuzzucoli Crucitti, M. Botta, R. Di Santo
Will integrase inhibitors be used as microbicides?
Current HIV Research, 2012, 10, 36-41. DOI: 10.2174/157016212799304706 (IF12 = 1.745)
2) D. De Vita, L. Scipione, S. Tortorella, P. Mellini, B. Di Rienzo, G. Simonetti, F. D. D’Auria, S. Panella, R Cirilli, R. Di Santo, A. T. Palamara
Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1phenylethanol derivatives.
Eur. J. Med. Chem. 2012, 49, 334-342. DOI: 10.1016/j.ejmech.2012.01.034 (IF12 = 3.346)
3) R. Fioravanti, I. Celestino, R. Costi, G. Crucitti Cuzzucoli, L. Pescatori, L. Mattiello, E. Novellino, P. Checconi, A.T. Palamara, L. Nencioni, R. Di Santo
Effects of polyphenol compounds on influenza A virus replication and definition of their mechanism of action
Bioorg. Med. Chem. 2012, 20, 5046-5052, DOI: 10.1016/j.bmc.2012.05.062 (IF12 = 2.921)
4) Mai, S. Valente, I. Lepore, C. Dell'Aversana, M. Tardugno, S. Castellano, G. Sbardella, S. Tomassi, S. Di Maro, E. Novellino, R. Di Santo, R. Costi, L. Altucci
Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells
Biochemie, 2012, 94, 2308-2313. DOI: 10.1016/j.biochi.2012.06.003 (IF12 = 3.022)
5) R. Di Santo, R. Costi, G. Cuzzucoli Crucitti, L. Pescatori, F. Rosi, L. Scipione, D. Celona, M. Vertechy, O. Ghirardi, P. Piovesan, M. Marzi, S. Caccia, G. Guiso, F. Giorgi, P. Minetti
Design, Synthesis and Structure-Activity Relationship of N-Aryl-Naphthylamine Derivatives as Amyloid Aggregation Inhibitors
J. Med. Chem. 2012, 55, 8538-8548. DOI: 10.1021/jm301105m (IF12 = 5.248)
6) G. Furlotti, M. A. Alisi, C. Apicella, A. Capezzone de Joannon, N. Cazzolla, R. Costi, G. Cuzzucoli Crucitti, B. Garrone, A. Iacovo, G. Magarò, G. Mangano, G. Miele, R. Ombrato, L. Pescatori, L. Polenzani, F. Rosi, M. Vitiello, R. Di Santo
Discovery and Pharmacological Profile of New 1H-Indazole-3-carboxamide and 2H-Pyrrolo[3,4-c]quinoline Derivatives as Selective Serotonin 4 Receptor Ligands
J. Med. Chem. 2012, 55, 9446-9466. DOI: 10.1021/jm300573d (IF12 = 5.248)
7) F. Rosi, G. Cuzzucoli Crucitti, A. Iacovo, G. Miele, L. Pescatori, R. Di Santo, R. Costi.
Convenient route to 2H-pyrrolo[3,4-b]quinolin-9(4H)-one skeleton via TosMIC reaction.
Synth. Commun. 2013, 1063-1072. DOI: 10.1080/00397911.2011.622062 (IF13 = 0.984)
8) L. Friggeri, F. Ballante, R. Ragno, I. Musmuca, D. De Vita, F. Manetti, M. Biava, L. Scipione, R. Di Santo, R. Costi, M. Feroci, S. Tortorella.
Pharmacophore assessment through 3-D QSAR: evaluation of the predictive ability on new derivatives by the application on a serie of antitubercular agents.
J. Chem. Inform. Mod. 2013, 53, 1463-1474, DOI: 10.1021/ci400132q (IF13 = 4.068)
9) L. Friggeri, L. Scipione, R. Costi, M. Kaiser, F. Moraca, C. Zamperini, B. Botta, R. Di Santo, D. De Vita, R. Brun, S. Tortorella.
New promising compounds with in vitro nanomolar activity against Trypanosoma cruzi.
ACS Med. Chem. Lett. 2013, 4, 538-541, DOI: 10.1021/ml400039r (IF13 = 3.073)
10) S. Taliani, I. Pugliesi, E. Barresi, S. Salerno, C. Marchand, K. Agama, F. Simorini, C. La Motta, A. M. Marini, F. S. Di Leva, L. Marinelli, S. Cosconati, E. Novellino, Y. Pommier, R. Di Santo, F. Da Settimo
Phenylpyrazolo[1,5‑a]quinazolin-5(4H)‑one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.
J. Med. Chem. 2013, 56, 7458−7462. DOI: 10.1021/jm400932c (IF13 = 5.480)
11) R. Costi, G. Cuzzucoli Crucitti, L. Pescatori, A. Messore, L. Scipione, S. Tortorella, A. Amoroso, E. Crespan, P. Campiglia, B. Maresca, A. Porta, I. Granata, E. Novellino, J. Gouge, M. Delarue, G. Maga, R. Di Santo.
New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: discovery, characterization, and crystal structure in complex with the target.
J. Med. Chem. 2013, 56, 7431-7441. DOI: 10.1021/jm4010187 (IF13 = 5.480)
12) R. Costi, M. Métifiot, F. Esposito, G. Cuzzucoli Crucitti, L. Pescatori, A. Messore, L. Scipione, S. Tortorella, L. Zinzula, E. Novellino, Y. Pommier, E. Tramontano, C. Marchand, R. Di Santo.
6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach.
J. Med. Chem. 2013, 56, 8588-8598. DOI: 10.1021/jm401040b. (IF13 = 5.480)
13) R. Di Santo.
Inhibiting the HIV integration process: past, present, and the future.
J. Med. Chem. 2014, 57, 539-566. DOI: 10.1021/jm400674a (IF14 = 5.447)
14) M. Feroci, I. Chiarotto, G. Forte, G. Simonetti, F. D. D’Auria, L. Maes, D. De Vita, L. Scipione, L. Friggeri, R. Di Santo, S. Tortorella.
Efficient electrochemical N-alkylation of N-Boc-protected 4-aminopyridines: towards new biologically active compounds.
ISRN Org. Chem. 2014, ID 621592. DOI: 10.1155/2014/621592
15) D. De Vita, L. Friggeri, F. Diodata D'Auria, F. Pandolfi, F. Piccoli, S. Panella, A. T. Palamara, G. Simonetti, L. Scipione, R. Di Santo, R. Costi, S. Tortorella.
Activity of caffeic acid derivatives against Candida albicans biofilm.
Bioorg. Med. Chem, Lett. 2014, 24, 1502-1505. DOI: 10.1016/j.bmcl.2014.02.005. (IF14 = 2.420)
16) R. Costi, M. Métifiot, S. Chung, G. Cuzzucoli Crucitti, K. Maddali, L. Pescatori, A. Messore, V. N. Madia, G. Pupo, L. Scipione, S. Tortorella, F. S. Di Leva, S. Cosconati, L. Marinelli, E. Novellino, S. F. J. Le Grice, A. Corona, Y. Pommier, C. Marchand, R. Di Santo
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase
J. Med. Chem. 2014, 57, 3223-3234. DOI: 10.1021/jm 5001503 (IF14 = 5.447)
17) F. Moraca, D. De Vita, F. Pandolfi, R. Di Santo, R. Costi, R. Cirilli, F. Diodata D'Auria, S. Panella, A. T. Palamara, G. Simonetti, M. Botta, L. Scipione.
Synthesis, biological evaluation and structure-activity correlation study of a series of imidazol-based compounds as Candida albicans inhibitors
Eur. J. Med. Chem. 2014, 83, 665-673. DOI: 10.1016/j.ejmech.2014.07.001 (IF14 = 3.447)
18) L. Friggeri, T. Y. Hargrove, G. Rachakonda, A. D. Williams, Z. Wawrzak, R. Di Santo, D. De Vita, M. R. Waterman, S. Tortorella, F. Villalta, G. I. Lepesheva.
Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14-demethylase: two regions of the enzyme molecule potentiate its inhibition
J. Med. Chem. 2014, 57, 6704-6717 DOI: 10.1021/jm500739f (IF14 = 5.447)
19) A. Corona, F. S. Di Leva, S. Tierry , L. Pescatori, G. Cuzzucoli Crucitti, F. Subra, O. Delelis, F. Esposito, G. Rigogliuso, R. Costi, S. Cosconati, E. Novellino, R. Di Santo, E. Tramontano.
Identification of highly conserved residues involved in the inhibition of the HIV-1 ribonuclease H function by diketoacid derivatives
Antimicrob. Ag. Chemother. 2014, 58, 6101-6110. DOI: 10.1128/AAC.03605-14 (IF14 = 4.476)
20) L. Friggeri, D. De Vita, F. Pandolfi, S. Tortorella, R. Costi, R. Di Santo, L. Scipione.
Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors.
J. Enzyme Inhib. Med. Chem. 2015, 30, 166-172. DOI: 10.3109/14756366.2013.866657. (IF14 = 2.332)
21) K. K. Das, N. Razzaghi-Asl, S. N. Tikare, R. Di Santo, R. Costi, A. Messore, L. Pescatori, G. Cuzzucoli Crucitti, J. G. Jargar, S. A. Dhundasi, L. Saso.
Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats.
J. Enzyme Inhib. Med. Chem. 2015, 30, in stampa, DOI: 10.3109/14756366.2015.1004061 (IF14 = 2.332)
22) M. D’Ascenzio, P. Chimenti, M. C. Gidaro, C. De Monte, D. De Vita, A. Granese, L. Scipione, R. Di Santo, G. Costa, S. Alcaro, M. Yáñez, S. Corradori
(Thiazol-2-yl)hydrazone derivatives from acetylpyridines as dual inhibitors of MAO and AChE: synthesis, biological evaluation and molecular modeling studies.
J. Enzyme Inhib. Med. Chem. 2015, 30, in stampa, DOI: 10.3109/14756366.2014.987138 (IF14 = 2.332)
23) G. Cuzzucoli Crucitti, M. Métifiot, L. Pescatori, A. Messore, V. N. Madia, G. Pupo, F. Saccoliti, L. Scipione, S. Tortorella, F. Esposito, A. Corona, M. Cadeddu, C. Marchand, Y. Pommier, E. Tramontano, R. Costi, R. Di Santo.
Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.
J. Med. Chem. 2015, 58, 1915-1928. DOI: 10.1021/jm501799k (IF14 = 5.447)
24) L. Pescatori, M. Métifiot, S. Chung, T. Masoaka, G. Cuzzucoli Crucitti, A. Messore, G. Pupo, V. N. Madia, F. Saccoliti, L. Scipione, S. Tortorella, F. S. Di Leva, S. Cosconati, L. Marinelli, E. Novellino, S. F. J. Le Grice, Y. Pommier, C. Marchand, R. Costi, R. Di Santo.
N-Substituted quinolinonyl diketo acid derivative sas HIV integrase strand transfer inhibitors and their activity against RNase H function of reverse transcriptase.
J. Med. Chem. 2015, 58, 4610-4623. DOI: 10.1021/acs.jmedchem.5b00159 (IF14 = 5.447)
25) G. Cuzzucoli Crucitti, L. Pescatori, A. Messore, V. N. Madia, G. Pupo, F. Saccoliti, L. Scipione, S. Tortorella, F. S. Di Leva, S. Cosconati, E. Novellino, Z. Debyser, F. Christ, R. Costi, R. Di Santo.
Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75
Eur. J. Med. Chem. 2015, 101, 288-294. DOI: 10.1016/j.ejmech.2015.06.036 (IF14 = 3.447)
26) J. Van Soom, G. Cuzzucoli Crucitti, R. Gladysz, P. Van der Veken, R. Di Santo, I. Stuyver, V. Buck, A.-M. Lambeir, V. Magdolen, J. Joossens, K. Augustyns.
The first potent diphenyl phosphonate K inhibitors with unexpected binding kinetics
MedChemCom 2015, 6, in stampa. DOI: 10.1039/C5MD00288E (IF14 = 2.495)
27) Ilari A, Pescatori L, Di Santo R, Battistoni A, Ammendola S, Falconi M, Berlutti F, Valenti P, Chiancone E. Salmonella enterica serovar Typhimurium growth is inhibited by the concomitant binding of Zn(II) and a pyrrolyl-hydroxamate to ZnuA, the soluble component of the ZnuABC transporter. Biochim Biophys Acta. 2016 Mar;1860(3):534-41. doi: 10.1016/j.bbagen.2015.12.006.
28) Schneider A, Corona A, Spöring I, Jordan M, Buchholz B, Maccioni E, Di Santo R, Bodem J, Tramontano E, Wöhrl BM. Biochemical characterization of a multi-drug resistant HIV-1 subtype AG reverse transcriptase: antagonism of AZT discrimination and excision pathways and sensitivity to RNase H inhibitors. Nucleic Acids Res. 2016 Mar 18;44(5):2310-22. doi: 10.1093/nar/gkw060.
29) De Vita D, Moraca F, Zamperini C, Pandolfi F, Di Santo R, Matheeussen A, Maes L, Tortorella S, Scipione L. In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51. Eur J Med Chem. 2016 May 4;113:28-33. doi: 10.1016/j.ejmech.2016.02.028.
30) Schmid T, Blees JS, Bajer MM, Wild J, Pescatori L, Cuzzucoli Crucitti G, Scipione L, Costi R, Henrich CJ, Brüne B, Colburn NH, Di Santo R. Diaryl Disulfides as Novel Stabilizers of Tumor Suppressor Pdcd4. PLoS One. 2016 Mar 16;11(3):e0151643. doi: 10.1371/journal.pone.0151643.
31) De Vita D, Pandolfi F, Cirilli R, Scipione L, Di Santo R, Friggeri L, Mori M, Fiorucci D, Maccari G, Arul Christopher RS, Zamperini C, Pau V, De Logu A, Tortorella S, Botta M. Discovery of in vitro antitubercular agents through in silico ligand-based approaches. Eur J Med Chem. 2016 Oct 4;121:169-80. doi: 10.1016/j.ejmech.2016.05.032.
32) De Vita D, Pandolfi F, Ornano L, Feroci M, Chiarotto I, Sileno I, Pepi F, Costi R, Di Santo R, Scipione L. New N,N-dimethylcarbamate inhibitors of acetylcholinesterase: design synthesis and biological evaluation. J Enzyme Inhib Med Chem. 2016; 31(sup4):106-113.
33) Corona A, di Leva FS, Rigogliuso G, Pescatori L, Madia VN, Subra F, Delelis O, Esposito F, Cadeddu M, Costi R, Cosconati S, Novellino E, Di Santo R, Tramontano E. New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H. Antiviral Res. 2016 Oct;134:236-243. doi: 10.1016/j.antiviral.2016.09.008.
34) De Vita D, Simonetti G, Pandolfi F, Costi R, Di Santo R, D'Auria FD, Scipione L. Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5931-5935. doi: 10.1016/j.bmcl.2016.10.091.
35) Saccoliti F, Angiulli G, Pupo G, Pescatori L, Madia VN, Messore A, Colotti G, Fiorillo A, Scipione L, Gramiccia M, Di Muccio T, Di Santo R, Costi R, Ilari A. Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives. J Enzyme Inhib Med Chem. 2017 Dec;32(1):304-310. doi: 10.1080/14756366.2016.1250755.
36) V. N. Madia, R. Benedetti, M. L. Barreca, L. Ngo, L. Pescatori, A. Messore, G. Pupo, F. Saccoliti, S. Valente, A. Mai, L. Scipione,Y. G. Zheng, C. Tintori, M. Botta, V. Cecchetti, L. Altucci, R. Di Santo, R. Costi.
Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase.
ChemMedChem. 2017, 12, 1359-1368. DOI: 10.1002/cmdc.201700040. (IF = 3.009)
37) F. Pandolfi, D. De Vita, M. Bortolami, A. Coluccia, R. Di Santo, R. Costi, V. Andrisano, F. Alabiso, C. Bergamini, R. Fato, M. Bartolini, L. Scipione.
New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation.
Eur. J. Med. Chem. 2017, 141, 197-210. DOI: 10.1016/j.ejmech.2017.09.022. (IF = 4.816)
38) D. De Vita, A. Angeli, F. Pandolfi, M. Bortolami, R. Costi, R. Di Santo, E. Suffredini, M. Ceruso, S. Del Prete, C. Capasso, L. Scipione, C. T. Supuran.
Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties.
J. Enzyme Inhib. Med. Chem. 2017, 32, 798-804.
DOI: 10.1080/14756366.2017.1327522. (IF = 3.638)
39) V. Poongavanam, A. Corona, C. Steinmann, L. Scipione, N. Grandi, F. Pandolfi, R. Di Santo, R. Costi, F. Esposito, E. Tramontano, J. Kongsted.
Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: binding mode insights through magnesium complexation and site-directed mutagenesis studies
MedChemCom 2018, 9. 562-575. DOI: 10.1039/c7md00600d. (IF17 = 2.343)
40) F. Saccoliti, V. N. Madia, V. Tudino, A. De Leo, L. Pescatori, A. Messore, D. De Vita, L. Scipione, R. Brun, M. Kaiser, P. Mäser, C. M. Calvet, G. K. Jenning, L. M. Podust, R. Costi, R. Di Santo.
Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents.
Eur. J. Med. Chem. 2018, 156, 53-60. DOI: 10.1016/j.ejmech.2018.06.063 (IF17 = 4.816)
41) V. N. Madia, A. Messore, L. Pescatori, F. Saccoliti, V. Tudino, A. De Leo, M. Bortolami, L. Scipione, R. Costi, S. Rivara, L. Scalvini, M. Mor, F. F. Ferrara, E. Pavoni, G. Roscilli, G. Cassinelli, F. M. Milazzo, G. Battistuzzi, R. Di Santo, G. Giannini.
Novel benzazole derivatives endowed with potent antiheparanase activity.
J. Med. Chem. 2018, 61, 6918-6936. DOI: 10.1021/acs.jmedchem.5b00159 (IF17 = 6.253)
42) A. Messore, V. N. Madia, L. Pescatori, F. Saccoliti, V. Tudino, A. De Leo, M. Bortolami, D. De Vita, L. Scipione, F. Pepi, R. Costi, S. Rivara, L. Scalvini, M. Mor, F. F. Ferrara, E. Pavoni, G. Roscilli, G. Cassinelli, F. M. Milazzo, G. Battistuzzi, R. Di Santo, G. Giannini.
Novel symmetrical benzazolyl derivatives endowed with potent anti-heparanase activity.
J. Med. Chem. 2018, 61, 6918-6936. DOI: 10.1021/acs.jmedchem.8b01497 (IF17 = 6.253)
43) V. N. Madia, A. Messore, L. Pescatori, F. Saccoliti, V. Tudino, A. De Leo, L. Scipione, L. Fiore, E. Rhoden, F. Manetti, M. S. Oberste, R. Di Santo, R. Costi.
In vitro antiviral activity of new oxazoline derivatives as potent poliovirus inhibitors.
J. Med. Chem. 2019, 62, 798-810. DOI: 10.1021/acs.jmedchem.8b01482 (IF17 = 6.253)
44) F. Saccoliti, V. N. Madia, V. Tudino, A. De Leo, L. Pescatori, A. Messore, D. De Vita, L. Scipione, R. Brun, M. Kaiser, P. Mäser, C. M. Calvet, G. K. Jennings, L. M. Podust, G. Pepe, R. Cirilli, C. Faggi, A. Di Marco, M. R. Battista, V. Summa, R. Costi, R. Di Santo.
Design, synthesis, and biological evaluation of new 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole derivatives as antiprotozoal agents.
J. Med. Chem. 2019, 62, 798-810. DOI: 10.1021/acs.jmedchem.8b01464 (IF17 = 6.253)
45) F. Pandolfi, F. D’Acierno, M.Bortolami, D. De Vita, R. Di Santo, R. Costi, G. Simonetti, L. Scipione.
Searching for new agents active against Candida albicans biofilm: A series of indole derivatives, design, synthesis and biological evaluation.
Eur. J. Med. Chem. 2019, 165, 93-106. DOI: 10.1016/j.ejmech.2019.01.012 (IF17 = 4.816)
46) V. Ruta, C. Longo, A. Boccaccini, V. N. Madia, F. Saccoliti, V. Tudino, R. Di Santo, R. Lorrai, R. Dello Ioio, S. Sabatini, R. Costi, P. Costantino, P. Vittorioso.
Inhibition of Polycomb Repressive Complex 2 activity reduces trimethylation of H3K27 and affects development in Arabidopsis seedlings.
BMC Plant Biol. 2019, 19, 429. DOI: 10.1186/s12870-019-2057-7. (IF18 = 3.930)
47) D. De Vita, A. Messore, C. Toniolo, C. Frezza, L. Scipione, C. M. Bertea, M. Micera, V. Di Sarno, V. N. Madia, I. Pindinello, P. Roscilli, A. Botto, G. Simonetti, A. Orekhova, S. Manfredini, R. Costi, R. Di Santo.
Towards a new application of amaranth seed oil as an agent against Candida albicans.
Nat Prod Res. 2019, EPub, DOI: 10.1080/14786419.2019.1696335. (IF18 = 1.928)
48) A. Messore, A. Corona, V. N. Madia, F. Saccoliti, V. Tudino, A. De Leo, L. Scipione, D. De Vita, G. Amendola, S. Di Maro, E. Novellino, S. Cosconati, M. Métifiot, M.-L. Andreola, P. Valenti, F. Esposito, N. Grandi, E. Tramontano, R. Costi, R. Di Santo.
Pyrrolyl pyrazoles as non-diketo acid inhibitors of the HIV-1 ribonuclease H function of reverse transcriptase.
ACS Med. Chem. Lett. 2020, 11, 798-805. DOI: 10.1021/acsmedchemlett.9b00617. (IF19 = 3.975)
49) V. N. Madia, A. Messore, F. Saccoliti, V. Tudino, A. De Leo, D. De Vita, M. Bortolami, L .Scipione, I. Pindinello, R. Costi, R. Di Santo.
Tegaserod for the Treatment of Irritable Bowel Syndrome.
Antiinflamm Antiallergy Agents Med Chem. 2020, 19, 342-369. DOI: 10.2174/1871523018666190911121306. (IF = )
50) G. Colotti, F. Saccoliti, M. Gramiccia, T. Di Muccio, J. Prakash, S. Yadav, V.K. Dubey, G. Vistoli, T. Battista, S. Mocci, A. Fiorillo, A. Bibi, V.N. Madia, A. Messore, R. Costi, R. Di Santo, A. Ilari. Structure-guided approach to identify a novel class of anti-leishmaniasis diaryl sulfide compounds targeting the trypanothione metabolism. Amino Acids 2020, 52, 247-259 DOI: 10.1007/s00726-019-02731-4. (IF19 = 3.063)
51) F. Esposito, M. Sechi, N. Pala, A. Sanna, P. C. Koneru, M. Kvaratskhelia, L. Naesens, A. Corona, N. Grandi, R. Di Santo, V. M. D'Amore, F. S. Di Leva, E. Novellino, S. Cosconati, E. Tramontano.
Discovery of dihydroxyindole-2-carboxylic acid derivatives as dual allosteric HIV-1 Integrase and Reverse Transcriptase associated Ribonuclease H inhibitors.
Antiviral Res. 2020, 174, 104671. DOI: 10.1016/j.antiviral.2019.104671. (IF19 = 4.101)
52) L. Taglieri, F. Saccoliti, A. Nicolai, G. Peruzzi, V.N. Madia, V. Tudino, A. Messore, R. Di Santo, M. Artico, S. Taurone, M. Salvati, R. Costi, S. Scarpa.
Discovery of a pyrimidine compound endowed with antitumor activity.
Invest. New Drugs 2020, 38, 39-49. DOI: 10.1007/s10637-019-00762-y. (IF19/20 = 3.525)
53) M. Bortolami, F. Pandolfi, D. De Vita, C. Carafa, A. Messore, R. Di Santo, M. Feroci, R. Costi, I. Chiarotto, D. Bagetta, , S. Alcaro, M. Colone, A. Stringaro, L. Scipione.
New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation.
Eur. J. Med. Chem. 2020, 198, 112350. DOI: 10.1016/j.ejmech.2020.112350. (IF19 = 5.572)
54) D. De Vita, V.N. Madia, V. Tudino, F. Saccoliti, A. De Leo, A. Messore, P. Roscilli, A. Botto, I. Pindinello, G. Santilli, L. Scipione, R. Costi, R. Di Santo.
Comparison of different methods for the extraction of cannabinoids from cannabis.
Natural Product Res. 2020, 34, 2952-2958. DOI: 10.1080/14786419.2019.1601194. (IF19 = 2.158)
55) F. Saccoliti, R. Di Santo, R. Costi.
Recent advancement in the search of innovative antiprotozoal agents targeting trypanothione metabolism.
ChemMedChem. 2020, 15, 2420-2435. DOI: 10.1002/cmdc.202000325 (IF19 = 3.124)
56) M. Bortolami, D. Rocco, A. Messore, R. Di Santo, R. Costi, V. N. Madia, L. Scipione, F. Pandolfi
Acetylcholinesterase inhibitors for the treatment of Alzheimer’s disease–a patent review (2016–present).
Expert Opin. Ther. Patents 2021, 31, 399-420. DOI: 10.1080/13543776.2021.1874344 (IF21= 6.674)
57) V. N. Madia, A. Nicolai, A. Messore, A. De Leo, D. Ialongo,V. Tudino, F. Saccoliti, D. De Vita, L. Scipione, M. Artico, S. Taurone, L. Taglieri, R. Di Santo, S. Scarpa, R. Costi
Design, synthesis and biological evaluation of new pyrimidine derivatives as anticancer agents
Molecules 2021, 26, 771. DOI: 10.3390/molecules26030771(IF21 = 4.411)
58) V. N. Madia, M. De Angelis, D. De Vita A. Messore, A. De Leo, D. Ialongo, V. Tudino, F. Saccoliti, G. De Chiara, S. Garzoli, L. Scipione, A. T. Palamara, R. Di Santo, L. Nencioni, R. Costi
Investigation of commiphora myrrha (Nees) Engl. oil and its main components for antiviral activity
Pharmaceuticals 2021, 14, 243. DOI: 10.3390/ph14030243 (IF21 = 5.863)
59) V. N. Madia, D. De Vita A. Messore, C. Toniolo, V. Tudino, A. De Leo, I. Pindinello, D. Ialongo, F. Saccoliti, A. M. D’Ursi, M. Grimaldi, P. Ceccobelli, L. Scipione, R. Di Santo, R. Costi
Analytical characterization of an inulin-type fructooligosaccharide from root-tubers of Asphodelus ramosus L.
Pharmaceuticals 2021, 14, 278. DOI: 10.3390/ph14030278 (IF21 = 5.863)
60) A. Nicolai, V. N. Madia, A. Messore, D. De Vita, A. De Leo, D. Ialongo, V. Tudino, E. Tortorella, L. Scipione, S. Taurone, T. Pergolizzi, M. Artico, R. Di Santo, R. Costi, S. Scarpa
Anti-tumoral effects of a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative on head and neck squamous carcinoma cell lines
Pharmaceuticals 2021, 14, 564. DOI: 10.3390/ph14060564 (IF21 = 5.863)
61) M. Bortolami, F. Pandolfi, A. Messore, D. Rocco, M. Feroci, R. Di Santo, D. De Vita, R. Costi, P. Cascarino, G. Simonetti, L. Scipione
Design, synthesis and biological evaluation of a series of iron and copper chelating deferiprone derivatives as new agents active against Candida albicans.
Bioorg. Med. Chem. Lett. 2021, 42, 128087. DOI: 10.1016/j.bmcl.2021.128087 (IF21 = 2.823)
62) A. Messore, A. Corona, V. N. Madia, F. Saccoliti, V. Tudino, A. De Leo, D. Ialongo, L. Scipione, D. De Vita, G. Amendola, E. Novellino, S. Cosconati, M. Métifiot, M.-L. Andreola, F. Esposito, N. Grandi, E. Tramontano, R. Costi, R. Di Santo.
Quinolinonyl non-diketo acid derivatives as inhibitors of HIV-1 ribonuclease H and polymerase functions of reverse transcriptase
J. Med. Chem. 2021, 64, 8579-8598. DOI: 10.1021/acs.jmedchem.1c00535 (IF21 = 7.446)
63) V. N. Madia, D. De Vita, D. Ialongo, V. Tudino, A. De Leo, L. Scipione, R. Di Santo, R. Costi, A. Messore.
Recent advances in recovery of lycopene from tomato waste: A potent antioxidant with endless benefits
Molecules 2021, 26, 4495. DOI: 10.3390/molecules26154495. (IF21 = 4.411)
64) A. Capozzi, G. Riitano, S. Recalchi, V. Manganelli, R. Costi, F. Saccoliti, F. Pulcinelli, T. Garofalo, R. Misasi, A. Longo, R. Di Santo, M. Sorice.
Effect of heparanase inhibitor on tissue factor overexpression in platelets and endothelial cells induced by anti-β2-GPI antibodies.
J. Thromb. Haemost. 2021, 19, 2302-2313. DOI: 10.1111/jth.15417. (IF21 = 5.824)
65) G. Amendola, B. Bocca, V. Picardo, P. Pelosi, B. Battistini, F. Ruggieri, D. Attard Barbini, D. De Vita, V. N. Madia, A. Messore, R. Di Santo, R. Costi.
Toxicological aspects of cannabinoid, pesticide and metal levels detected in light Cannabis inflorescences grown in Italy
Food Chem. Toxicol. 2021, 156, 112447. DOI: 10.1016/j.fct.2021.112447. (IF21 = 6.023)
66) S. Ammendola, V. Secli, F. Pacello, M. Bortolami, F. Pandolfi, A. Messore, R. Di Santo, L. Scipione, A. Battistoni
Salmonella typhimurium and pseudomonas aeruginosa respond differently to the Fe chelator deferiprone and to some novel deferiprone derivatives
Int. J. Mol. Sci. 2021, 22, 10217. DOI: 10.3390/ijms221910217 (IF21 = 6.208)
67) M. Bortolami, F. Pandolfi, V. Tudino, A. Messore, V. N. Madia, D. De Vita, R. Di Santo, R. Costi, I. Romeo, S. Alcaro, M. Colone, A. Stringaro. A. Espargaro, R. Sabatè, L. Scipione
New Pyrimidine and Pyridine Derivatives as Multitarget Cholinesterase Inhibitors: Design, Synthesis, and in Vitro and in Cellulo Evaluation
ACS Chemical Neurosci. 2021, 12, 4090-4112. DOI: 10.1021/acschemneuro.1c00485 (IF = 4.418)
68) D. Boi, F. Souvalidou, D. Capelli, F. Polverino, G. Marini, R. Montanari, G. Pochetti, A. Tramonti, R. Contestabile, D. Trisciuoglio , P. Carpinelli , C. Ascanelli, C. Lindon, A. De Leo, M. Saviano, R. Di Santo, R. Costi, G. Guarguaglini, A. Paiardini
PHA-680626 Is an Effective Inhibitor of the Interaction between Aurora-A and N-Myc
Int. J. Mol. Sci. 2021, 22, 13122; DOI: 10.3390/ijms222313122 (IF = 5.924)
69) V. N. Madia, A. Messore, A. De Leo, V. Tudino, I. Pindinello, F. Saccoliti, D. De Vita, L. Scipione, R. Costi, R. Di Santo
Small-molecule inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H function: Challenges and recent developments.
Curr. Med. Chem. 2021, 28, 6146 – 6178. DOI: 10.2174/0929867328666210322164557 (IF = 4.53).
70) C. O. Vaso, N. M. Bila, F. Pandolfi, D. De Vita, M. Bortolami, J. L. C. Bonatti, R. A. de Moraes Silva, L. N. C. Goncalves, V. Tudino, R. Costi, R. Di Santo, M. J. S. Mendes-Giannini, C. B. Costa-Orlandi, L. Scipione, A. M. Fusco-Almeida
Evaluation of the Anti-Histoplasma capsulatum Activity of Indole and Nitrofuran Derivatives and Their Pharmacological Safety in Three-Dimensional Cell Cultures
Pharmaceutics 2022, 14, 1043. DOI: 10.3390/pharmaceutics14051043. (IF21 = 6.525)
71) V. N. Madia, W. Toscanelli, D. De Vita, M. De Angelis, A. Messore, D. Ialongo, L. Luigi, V. Tudino, F. D. D’auria, R. Di Santo, S. Garzoli, A. Stringaro, M. Colone, M. Marchetti, F. Superti, L. Nencioni, R. Costi
Ultrastructural Damages to H1N1 Influenza Virus Caused by Vapor Essential Oils
Molecules 2022, 27, 3718. DOI: 10.3390/molecules27123718. (IF21 = 4.927)
72) M. Bortolami, F. Pandolfi, V. Tudino, A. Messore, V. N. Madia, D. De Vita, R. Di Santo, R. Costi, I. Romeo, S. Alcaro, M. Colone, A. Stringaro, A. Espargarò, R. Sabatè, L. Scipione
Design, Synthesis, and In Vitro, In Silico and In Cellulo Evaluation of New Pyrimidine and Pyridine Amide and Carbamate Derivatives as Multi-Functional Cholinesterase Inhibitors
Pharmaceuticals 2022, 15, 673. DOI: 10.3390/ph15060673. (IF21 = 5.215)
73) C. Longo, A. Lepri, A. Paciolla, A. Messore, D. De Vita, M. C. Bonaccorsi di Patti, M. Amadei, V. N. Madia, D. Ialongo, R. Di Santo, R. Costi, P. Vittorioso
New Inhibitors of the Human p300/CBP Acetyltransferase Are Selectively Active against the Arabidopsis HAC Protein
Int. J. Mol. Sci. 2022, 23, 10446. DOI: 10.3390/ijms231810446 (IF21 = 6.208)

Books (Chapters)

1) Foye’s Principi di Chimica Farmaceutica. Piccin – Capitolo 40 Antifungini. Traduzione. Quinta edizione Italiana sulla sesta americana (2009)
2) Foye’s Principi di Chimica Farmaceutica Piccin – Capitolo 45 La salute dell’uomo. Traduzione. Quinta edizione Italiana sulla sesta americana (2009)
3) Foye’s Principi di Chimica Farmaceutica Piccin – Capitolo 46 La salute della donna. Traduzione. Quinta edizione Italiana sulla sesta americana (2009)
4) Foye’s Principi di Chimica Farmaceutica Piccin – Capitolo 35 Antifungini. Traduzione. Sesta edizione Italiana sulla settima americana (2014)
5) Foye’s Principi di Chimica Farmaceutica Piccin – Capitolo 40 La salute dell’uomo. Traduzione. Sesta edizione Italiana sulla settima americana (2014)
6) Foye’s Principi di Chimica Farmaceutica Piccin – Capitolo 41 La salute della donna. Traduzione. Sesta edizione Italiana sulla settima americana (2014)
7) Chimica Farmaceutica. A. Gasco, F. Gualtieri, C. Melchiorre. Casa Editrice Ambrosiana. Capitolo 18 Ipotensivi. (2015)
8) Foye’s Essentials Principi di Chimica Farmaceutica Piccin – Capitolo 15 Antiiperlipidemici. Traduzione. Prima edizione Italiana (2016)
9) Chimica Farmaceutica. A. Gasco, F. Gualtieri, C. Melchiorre. Casa Editrice Ambrosiana. 2a Ed Capitolo 18 Ipotensivi. (2019)