DAVIDE IALONGO

Dottore di ricerca

ciclo: XXXVI


supervisore: Roberta Costi
relatore: Roberta Costi
co-supervisore: Roberta Costi

Titolo della tesi: Design, synthesis and biological evaluation of new heterocycles endowed with antitumoral activity

My Ph.D. thesis is focused on the design and synthesis of new heterocycle-based small molecules endowed with antitumoral activity. Heparanase inhibitors The first part of my thesis is focused on Heparanase (Hpse), the sole mammalian enzyme able to cleave glycosaminoglycan heparan sulfate side chains of heparan sulfate proteoglycans, with retention of the anomeric configuration. Proteoglycans participate in several biological activities by interacting with various enzymes or receptors. By editing their structures, Hpse is consequently involved in a multitude of vital cellular pathways, but its aberrant activity is associated with tumor development and negative prognosis. Indeed, it contributes to all known hallmarks of cancer, thus making it an attractive pharmacological target. However, although the interest in this enzyme is enormously grown in the past years and various attempts have been made to develop new Hpse inhibitors, to date no Hpse small-molecule-based inhibitors have ever entered clinical trials. Hence, I designed and synthesized two libraries of benzimidazole- and benzoxazole-based molecules, characterized by both symmetrical and asymmetrical structures. These molecules were conceived by merging the pharmacophoric moieties of known Hpse small-molecule-based in vitro inhibitors and by functionalizing the terminal 5-acetyl groups with amino acids or amino alkyl boronic groups. Fluorine-hydrogen atom substitutions were also evaluated in the central aniline rings, and both ureidic and thioureidic central groups were synthesized. The majority of newly synthesized compounds were found active in in vitro Hpse inhibition assays with micromolar concentrations, with symmetric compounds showing the better potencies. Among them, a glycine conjugated thiourea benzoxazole exhibited the best inhibitory activity found, with an IC50 of 80 nM. By comparing the activity of this compound to that of the polysaccharide roneparstat, one of the most potent Hpse inhibitors reported, is evident that, although the newly synthesized thioureidic benzoxazole is 16 times less potent than roneparstat if the activity is expressed in molar concentration, the amount potentially necessary for its clinical use could be about the half of that of roneparstat due to their huge difference in molecular weight, highlighting the great versatility and suitability of small molecules in the development of new Hpse inhibitors. Through computational studies, new compounds were demonstrated to act as orthosteric competitive inhibitors, lying within the Hpse substrate binding cleft and occupying the catalytic site. Heparin binding domain 2 (HBD-2) appears as the major anchoring point for the amino acids asymmetric benzazoles, while the symmetric compounds place the urea or thiourea group close to the catalytic residue E225 and contact both the Hpse HBD-1 and HBD-2, thus undertaking a higher number of polar interactions. Furthermore, some compounds proved also to inhibit cell proliferation and invasive potential on HT1080, U87MG and U2OS tumor cell lines and the transcription of genes encoding for proangiogenic factors, such as MMP-9, VEGF, and FGFs in tumor cells. More in detail, in U87MG cell line, the most potent Hpse inhibitor found was also demonstrated to induce the autophagosomes accumulation and the arrest in the autophagic flux. Consistently, the treatment with the newly synthesized inhibitor might compromise the pro-autophagy function of the intracellular Hpse, considering the ability of the inhibitor to easily cross the cellular plasma membrane. Protein kinase inhibitors The second part of my thesis regards the design and synthesis of new series of small-molecule protein kinase inhibitors. Protein kinases catalyze the transfer of γ-phosphates from ATP to an amino acid -OH group of a substrate protein, and according to the amino acid nature, they could be classified as serine/threonine or tyrosine protein kinases. Protein kinases are intimately involved in many physiological activities, but their deregulation has widely recognized to be a relevant mechanism by which cancer cells evade normal constraints and adopt tumorigenic properties. Hence, the discovery of protein kinases inhibitors has become one of the most intensively pursued classes of recent drugs, capturing funding for billions of dollars worldwide. In this field, pyrimidines have received much interest due to their intrinsic biological potential and many pyrimidine-based derivatives possess promising anticancer activity thanks to the inhibition of the protein kinases catalytic site. In this context, I designed and synthesized two classes of compounds, 2,4,6-tris-amino pyrimidines and 2-anilino pyrimidines. A 2,4,6-tris-amino pyrimidine derivative was previously identified as an inhibitor of replication, a negative regulator of cell cycle progression and an inducer of apoptosis in U87MG, MDA-MB231, and HT-29 cell histotypes. In order to verify if the mechanism of action of this compound is due to a protein kinase inhibition and to investigate the SAR, new structurally related derivatives were conceived by carrying out substitutions in position 6 of the pyrimidine core and/or on the 2-aniline ring and by derivatizing the 2-NH- group of pyrimidine with a p-fluorobenzyl ring. The new N-benzylated compounds proved to be generally endowed with higher potencies than the hit compound, by causing a more pronounced decrease in cell viability. The best acting compound reported EC50 values ranging from 10 to 26 μM at 24 h of treatment and from 5 to 8 μM at 48 h of treatment, 13-fold higher than the starting compound, against all the tested cell lines. Among this series, considering the substitution in meta position of aniline ring, propanediamine derivatives activities decreased in the following order: Cl > F > NO2 ≈ OCH3, indicating the importance of an electron withdrawing group. These compounds were also tested to verify their protein kinases inhibition activities by HTRF assay, and they were found to hinder EGFR, wt and mutated isoforms, with nanomolar activities. The 2-anilino pyrimidines, instead, were tailor-designed to mostly interact with Aurora kinases A (AURKA). More in detail, I investigated and expanded this scaffold by studying three sub-classes of compounds: (1) 4-(pyrimidin-2-ylamino)benzoic acids, to be orthosteric competitive inhibitors of AURKA; (2) protein-protein interaction inhibitors of AURKA/N-Myc interaction, characterized by an AURKA orthosteric competitive core and an electrophilic warhead to covalently bind to the AURKA Cys290 in order to induce an AURKA conformational change to prevent N-Myc binding; and (3) dual kinases inhibitors, of AURKA and HDAC, merging the structures of previously AURKA inhibitors identified and HDAC inhibitor quisinostat. All the newly designed compounds were synthesized and evaluated to inhibit AURKA in in vitro ADP-Glo assay. The majority of compounds were found active with nanomolar concentration and most of them were also co-crystallized in the active site of the enzyme. Considering the second group of compounds, fumaric acid derivative inhibited AURKA and also other kinases, namely c-KIT, PDGFR wt and mutated isoforms and VEGFR2, in in vitro HTRF assay, emerging as an innovative chemical scaffold for the development of a new pluri-kinase inhibitor, particularly useful for those disease in which PDGFR and VEGRF2 cooperate to overcome Bevacizumab efficacy. Anyway, other biological studies to evaluate the AURKA/N-Myc interaction inhibition and the covalent-binding capabilities are under investigation. Regarding the last group of protein inhibitors, while the benzoic acid derivative inhibited AURKA in concentrations lower than every other AURKA inhibitor to date described, the hydroxamic acid counterparts showed lower AURKA inhibition activities but, at the same time, micromolar HDAC inhibition values, acting as potential dual kinases inhibitors. To conclude, in this Ph.D. thesis, I designed and synthesized two libraries of compounds. Benzimidazole- and benzoxazole-based molecules were found active against Hpse, in in vitro assays, with symmetric derivatives showing the best potencies. Moreover, they also inhibited cell proliferation, invasive potential, and the transcription of several pro-tumorigenic genes in the tested cancer lines, and act as a balance between autophagy and apoptosis. Considering the pyrimidine-based compounds, the first group of newly designed and synthesized N-benzylated 2,4,6-trisubstitued pyrimidines functions as antitumoral compounds on various tested cell lines and exerted pronounced EGFR wt and mutated isoforms inhibition activities. The 2-anilino pyrimidine, instead, act as AURKA orthosteric inhibitors, and their chemical tailored-modifications allow to selective modulate their activity profile, spacing from the pluri-kinase inhibitor fumaric acid to the dual AURKA/HDAC inhibitors. The most promising compounds lend themselves to be optimized to further hit-to-lead development processes.

Produzione scientifica

11573/1697149 - 2023 - New blood-brain-barrier permeable compounds as Naegleria Fowleri CYP51 inhibitors.
Arpacioglu, M.; Madia, V. N.; Ialongo, D.; Patacchini, E.; Messore, A.; Tudino, V.; Sharma, V.; Nguyen, J.; Debnath, A.; Podust, L.; Palenca, I.; Basili Franzin, S.; Seguella, L.; Esposito, G.; Petrucci, R.; Di Matteo, P.; Bortolami, M.; Scipione, L.; Costi, R.; Di Santo, R. - 04f Poster
congresso: XXVIII edition of the National Meeting on Medicinal Chemistry (Chieti; Italy)
libro: XXVIII edition of the National Meeting on Medicinal Chemistry - ()

11573/1697156 - 2023 - Novel nsp13 inhibitors capable of blocking viral replication of SARS-CoV-2.
Arpacioglu, M.; Madia, V. N.; Messore, A.; Patacchini, E.; Ialongo, D.; Tudino, V.; Scipione, L.; Corona, A.; Esposito, F.; Artico, M.; Amatore, D.; Faggioni, G.; De Santis, R.; Lista, F.; Tramontano, E.; Costi, R.; Di Santo, R. - 04f Poster
congresso: ESMEC 2023 - European School of Medicinal Chemistry – 42nd Edition (Urbino; Italy)
libro: ESMEC 2023 - European School of Medicinal Chemistry – 42nd Edition - ()

11573/1686714 - 2023 - Diketo acid inhibitors of nsp13 of SARS-CoV-2 block viral replication
Corona, Angela; Madia, Valentina Noemi; De Santis, Riccardo; Manelfi, Candida; Emmolo, Roberta; Ialongo, Davide; Patacchini, Elisa; Messore, Antonella; Amatore, Donatella; Faggioni, Giovanni; Artico, Marco; Iaconis, Daniela; Talarico, Carmine; Di Santo, Roberto; Lista, Florigio; Costi, Roberta; Tramontano, Enzo - 01a Articolo in rivista
rivista: ANTIVIRAL RESEARCH (Amsterdam: Elsevier Science) pp. - - issn: 1872-9096 - wos: WOS:001062175600001 (0) - scopus: 2-s2.0-85167598331 (1)

11573/1697165 - 2023 - Aminopyrimidine derivatives as new protein kinase inhibitors endowed with anticancer activity.
Ialongo, D.; Madia, V. N.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Scarpa, S.; Rauh, D; Di Santo, R.; Costi, R. - 04f Poster
congresso: 10th EFMC Young Medicinal Chemists' Symposium (Zagreb; Croatia.)
libro: 10th EFMC Young Medicinal Chemists' Symposium - ()

11573/1697174 - 2023 - Pyrimidine-based compounds as new promising protein kinase inhibitors for cancer treatment.
Ialongo, D.; Madia, V. N.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Scarpa, S.; Rauh, D; Di Santo, R.; Costi, R. - 04f Poster
congresso: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (Zagreb; Croatia.)
libro: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry - ()

11573/1697175 - 2023 - Diketo acid heterocyclic derivatives as new SARS-CoV-2 nsp13 inhibitors blocking viral replication.
Ialongo, D.; Madia, V. N.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Tudino, V.; Scipione, L.; Corona, A.; Esposito, F.; Artico, M.; Amatore, D.; Faggioni, G.; De Santis, R.; Lista, F.; Tramontano, E.; Costi, R.; Di Santo, R. - 04f Poster
congresso: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (Zagreb; Croatia.)
libro: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry - ()

11573/1697147 - 2023 - Identification of novel aminopyrimidine derivatives as protein kinase inhibitors blocking cell growth.
Ialongo, Davide; Madia, Valentina Noemi; Messore, Antonella; Patacchini, Elisa; Arpacioglu, Merve; Scipione, Luigi; Scarpa, S.; Rauh, D.; Di Santo, R.; Costi, R. - 04f Poster
congresso: XXVIII edition of the National Meeting on Medicinal Chemistry (Chieti; Italy)
libro: XXVIII edition of the National Meeting on Medicinal Chemistry - ()

11573/1697162 - 2023 - New diketo acid derivatives as dual SARS-CoV-2 nsp13 inhibitors active against viral replication.
Ialongo, Davide; Madia, Valentina Noemi; Messore, Antonella; Patacchini, Elisa; Arpacioglu, Merve; Tudino, Valeria; Scipione, Luigi; Corona, Angela; Esposito, Francesca; Artico, Marco; Amatore, Donatella; Faggioni, Giovanni; De Santis, Riccardo; Lista, Florigio; Tramontano, Enzo; Costi, Roberta; Di Santo, Roberto - 04f Poster
congresso: 10th EFMC Young Medicinal Chemists' Symposium (Zagreb; Croatia.)
libro: 10th EFMC Young Medicinal Chemists' Symposium - ()

11573/1668131 - 2023 - Pyrrolyl and indolyl α-γ-diketo acid derivatives acting as selective inhibitors of human carbonic anhydrases IX and XII
Ialongo, Davide; Messore, Antonella; Madia, Valentina Noemi; Tudino, Valeria; Nocentini, Alessio; Gratteri, Paola; Giovannuzzi, Simone; Supuran, Claudiu T.; Nicolai, Alice; Scarpa, Susanna; Taurone, Samanta; Camarda, Michele; Artico, Marco; Papa, Veronica; Saccoliti, Francesco; Scipione, Luigi; Di Santo, Roberto; Costi, Roberta - 01a Articolo in rivista
rivista: PHARMACEUTICALS (Basel : MDPI, Molecular Diversity Preservation International, 2004-) pp. - - issn: 1424-8247 - wos: WOS:000941695000001 (2) - scopus: 2-s2.0-85148943598 (2)

11573/1684012 - 2023 - Synergistic Effects of Caffeine in Combination with Conventional Drugs: Perspectives of a Drug That Never Ages
Ialongo, Davide; Tudino, Valeria; Arpacioglu, Merve; Messore, Antonella; Patacchini, Elisa; Costi, Roberta; Di Santo, Roberto; Madia, Valentina Noemi - 01g Articolo di rassegna (Review)
rivista: PHARMACEUTICALS (Basel : MDPI, Molecular Diversity Preservation International, 2004-) pp. 730- - issn: 1424-8247 - wos: WOS:000997931100001 (2) - scopus: 2-s2.0-85160675541 (4)

11573/1697142 - 2023 - Discovery of new small molecules as anti-SARS-CoV-2 agents inhibiting ACE2-spike binding.
Madia, V. N.; Ialongo, D.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Di Santo, R.; Costi, R. - 04f Poster
congresso: XXVIII edition of the National Meeting on Medicinal Chemistry (Chieti; Italy)
libro: XXVIII edition of the National Meeting on Medicinal Chemistry - ()

11573/1697168 - 2023 - Dual HIV-1 integrase catalytic site and integrase-RNA interaction inhibitors.
Madia, V. N.; Ialongo, D.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Kvaratskhelia, M.; Di Santo, R.; Costi, R. - 04f Poster
congresso: 10th EFMC Young Medicinal Chemists' Symposium (Zagreb; Croatia.)
libro: 10th EFMC Young Medicinal Chemists' Symposium - ()

11573/1697179 - 2023 - Quinolinonyl derivatives as dual inhibitors of the HIV-1 integrase catalytic site and integrase-RNA interactions.
Madia, V. N.; Ialongo, D.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Kvaratskhelia, M.; Di Santo, R.; Costi, R. - 04f Poster
congresso: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (Zagreb; Croatia.)
libro: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry - ()

11573/1697181 - 2023 - Design and synthesis of brain permeable anti-Naegleria fowleri agents targeting CYP51 for primary amoebic meningoencephalitis treatment.
Madia, V. N.; Ialongo, D.; Messore, A.; Patacchini, E.; Arpacioglu, M.; Tudino, V.; Sharma, V.; Nguyen, J.; Debnath, A.; Podust, L.; Palenca, I.; Basili Franzin, S.; Seguella, L.; Esposito, G.; Petrucci, R.; Di Matteo, P.; Bortolami, M.; Scipione, L.; Costi, R.; Di Santo, R. - 04f Poster
congresso: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (Zagreb; Croatia.)
libro: IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry - ()

11573/1697153 - 2023 - Small molecule derivatives as dual inhibitors of SARS-CoV-2 nsp13 blocking viral replication.
Madia, V. N.; Ialongo, D.; Patacchini, E.; Arpacioglu, M.; Messore, A.; Tramontano, E.; De Santis, R.; Lista, F.; Costi, R.; Di Santo, R. - 04f Poster
congresso: 3rd Synthesis in Drug Discovery and Development (Virtual meeting)
libro: 3rd Synthesis in Drug Discovery and Development - ()

11573/1697146 - 2023 - Discovery of quinolinonyl derivatives as anti-HIV-1 inhibitors endowed with an innovative mechanism of action.
Madia, Valentina Noemi; Ialongo, Davide; Messore, Antonella; Patacchini, Elisa; Arpacioglu, Merve; Scipione, Luigi; Di Santo, Roberto; And Costi, Roberta. - 04f Poster
congresso: XXVIII edition of the National Meeting on Medicinal Chemistry (Chieti; Italy)
libro: XXVIII edition of the National Meeting on Medicinal Chemistry - ()

11573/1663401 - 2023 - Inhibition of Leishmania infantum Trypanothione Reductase by New Aminopropanone Derivatives Interacting with the NADPH Binding Site
Madia, Valentina Noemi; Ialongo, Davide; Patacchini, Elisa; Exertier, Cécile; Antonelli, Lorenzo; Colotti, Gianni; Messore, Antonella; Tudino, Valeria; Saccoliti, Francesco; Scipione, Luigi; Ilari, Andrea; Costi, Roberta; Di Santo, Roberto Di - 01a Articolo in rivista
rivista: MOLECULES (Basel: MDPI Berlin: Springer, 1996-) pp. 338- - issn: 1420-3049 - wos: WOS:000909976300001 (1) - scopus: 2-s2.0-85145692255 (1)

11573/1697172 - 2023 - Miconazole-like compounds as brain permeable anti-Naegleria Fowleri agents targeting CYP51.
Madia, Valentina Noemi; Ialongo, Davide; Patacchini, Elisa; Messore, Antonella; Arpacioglu, Merve; Tudino, V.; Sharma, V.; Nguyen, J.; Debnath, A.; Podust, L.; Palenca, I.; Basili Franzin, S.; Seguella, L.; Esposito, G.; Petrucci, R.; Di Matteo, P.; Bortolami, M.; Scipione, L.; Costi, Roberta; Di Santo, Roberto. - 04f Poster
congresso: 10th EFMC Young Medicinal Chemists' Symposium (Zagreb; Croatia.)
libro: 10th EFMC Young Medicinal Chemists' Symposium - ()

11573/1687531 - 2023 - Role of a Novel Heparanase Inhibitor on the Balance between Apoptosis and Autophagy in U87 Human Glioblastoma Cells
Manganelli, V.; Misasi, R.; Riitano, G.; Capozzi, A.; Mattei, V.; Caglar, T. R.; Ialongo, D.; Madia, V. N.; Messore, A.; Costi, R.; Di Santo, R.; Sorice, M.; Garofalo, T. - 01a Articolo in rivista
rivista: CELLS (Basel: mdpi-Molecular Diversity Preservation International) pp. 1-14 - issn: 2073-4409 - wos: WOS:001038054000001 (1) - scopus: 2-s2.0-85165884087 (1)

11573/1697140 - 2023 - Design and synthesis of tetrahydro-β-carbolines derivatives as PDIA inhibitors.
Messore, A.; Madia, V. N.; Ialongo, D.; Patacchini, E.; Arpacioglu, M.; Scipione, L.; Altieri, F.; Paglia, G.; Meschiari, G.; Di Santo, R.; Costi, R. - 04f Poster
congresso: XXVIII edition of the National Meeting on Medicinal Chemistry (Chieti; Italy)
libro: XXVIII edition of the National Meeting on Medicinal Chemistry - ()

11573/1697150 - 2023 - From Iloperidone to new Sigma1 agonists: a structure-based approach for Huntington's disease treatment.
Patacchini, Elisa; Madia, Valentina Noemi; Ialongo, Davide; Messore, Antonella; Ilari, Andrea; Cosconati, Sandro; Di Santo, Roberto; Costi, Roberta. - 04f Poster
congresso: ESMEC 2023 - European School of Medicinal Chemistry – 42nd Edition (Urbino; Italy)
libro: ESMEC 2023 - European School of Medicinal Chemistry – 42nd Edition - ()

11573/1696092 - 2023 - Miconazole-like Scaffold is a Promising Lead for Naegleria fowleri-Specific CYP51 Inhibitors
Sharma, Vandna; Madia, Valentina Noemi; Tudino, Valeria; V Nguyen, Jennifer; Debnath, Anjan; Messore, Antonella; Ialongo, Davide; Patacchini, Elisa; Palenca, Irene; Basili Franzin, Silvia; Seguella, Luisa; Esposito, Giuseppe; Petrucci, Rita; Di Matteo, Paola; Bortolami, Martina; Saccoliti, Francesco; Di Santo, Roberto; Scipione, Luigi; Costi, Roberta; M Podust, Larissa - 01a Articolo in rivista
rivista: JOURNAL OF MEDICINAL CHEMISTRY (Washington, DC: American Chemical Society) pp. 17059-17073 - issn: 0022-2623 - wos: WOS:001134079100001 (0) - scopus: 2-s2.0-85180091142 (0)

11573/1654141 - 2022 - New Inhibitors of the human p300/CBP acetyltransferase are selectively active against the Arabidopsis HAC proteins
Longo, Chiara; Lepri, Andrea; Paciolla, Andrea; Messore, Antonella; De Vita, Daniela; Bonaccorsi Di Patti, Maria Carmela; Amadei, Matteo; Madia, Valentina Noemi; Ialongo, Davide; Di Santo, Roberto; Costi, Roberta; Vittorioso, Paola - 01a Articolo in rivista
rivista: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (Basel: MDPI Center) pp. 1-18 - issn: 1422-0067 - wos: WOS:000859422800001 (3) - scopus: 2-s2.0-85138734584 (3)

11573/1648549 - 2022 - Ultrastructural damages to H1N1 influenza virus caused by vapor essential oils
Madia, Valentina Noemi; Toscanelli, Walter; De Vita, Daniela; De Angelis, Marta; Messore, Antonella; Ialongo, Davide; Scipione, Luigi; Tudino, Valeria; D'auria, Felicia Diodata; Di Santo, Roberto; Garzoli, Stefania; Stringaro, Annarita; Colone, Marisa; Marchetti, Magda; Superti, Fabiana; Nencioni, Lucia; Costi, Roberta - 01a Articolo in rivista
rivista: MOLECULES (Basel: MDPI Berlin: Springer, 1996-) pp. 1-14 - issn: 1420-3049 - wos: WOS:000816243700001 (6) - scopus: 2-s2.0-85131746075 (7)

11573/1540215 - 2021 - Investigation of Commiphora myrrha (Nees) Engl. oil and its main components for antiviral activity
Madia, Valentina Noemi; De Angelis, Marta; De Vita, Daniela; Messore, Antonella; De Leo, Alessandro; Ialongo, Davide; Tudino, Valeria; Saccoliti, Francesco; De Chiara, Giovanna; Garzoli, Stefania; Scipione, Luigi; Palamara, Anna Teresa; Di Santo, Roberto; Nencioni, Lucia; Costi, Roberta - 01a Articolo in rivista
rivista: PHARMACEUTICALS (Basel : MDPI, Molecular Diversity Preservation International, 2004-) pp. - - issn: 1424-8247 - wos: WOS:000634055800001 (16) - scopus: 2-s2.0-85102987115 (20)

11573/1564144 - 2021 - Recent advances in recovery of lycopene from tomato waste. A potent antioxidant with endless benefits
Madia, Valentina Noemi; De Vita, Daniela; Ialongo, Davide; Tudino, Valeria; De Leo, Alessandro; Scipione, Luigi; Di Santo, Roberto; Costi, Roberta; Messore, Antonella - 01a Articolo in rivista
rivista: MOLECULES (Basel: MDPI Berlin: Springer, 1996-) pp. 1-18 - issn: 1420-3049 - wos: WOS:000682223800001 (38) - scopus: 2-s2.0-85111602310 (46)

11573/1540619 - 2021 - Analytical characterization of an inulin-type fructooligosaccharide from root-tubers of Asphodelus ramosus L
Madia, Valentina Noemi; De Vita, Daniela; Messore, Antonella; Toniolo, Chiara; Tudino, Valeria; De Leo, Alessandro; Pindinello, Ivano; Ialongo, Davide; Saccoliti, Francesco; D'ursi, Anna Maria; Grimaldi, Manuela; Ceccobelli, Pietro; Scipione, Luigi; Di Santo, Roberto; Costi, Roberta - 01a Articolo in rivista
rivista: PHARMACEUTICALS (Basel : MDPI, Molecular Diversity Preservation International, 2004-) pp. - - issn: 1424-8247 - wos: WOS:000634075100001 (5) - scopus: 2-s2.0-85103099178 (4)

11573/1493998 - 2021 - Design, synthesis and biological evaluation of new pyrimidine derivatives as anticancer agents
Madia, Valentina Noemi; Nicolai, Alice; Messore, Antonella; De Leo, Alessandro; Ialongo, Davide; Tudino, Valeria; Saccoliti, Francesco; De Vita, Daniela; Scipione, Luigi; Artico, Marco; Taurone, Samanta; Taglieri, Ludovica; Di Santo, Roberto; Scarpa, Susanna; Costi, Roberta - 01a Articolo in rivista
rivista: MOLECULES (Basel: MDPI Berlin: Springer, 1996-) pp. - - issn: 1420-3049 - wos: WOS:000615455300001 (14) - scopus: 2-s2.0-85101195321 (16)

11573/1556284 - 2021 - Quinolinonyl non-diketo acid derivatives as Inhibitors of HIV-1 ribonuclease H and polymerase functions of reverse transcriptase
Messore, Antonella; Corona, Angela; Madia, Valentina Noemi; Saccoliti, Francesco; Tudino, Valeria; De Leo, Alessandro; Ialongo, Davide; Scipione, Luigi; De Vita, Daniela; Amendola, Giorgio; Novellino, Ettore; Cosconati, Sandro; Métifiot, Mathieu; Andreola, Marie-Line; Esposito, Francesca; Grandi, Nicole; Tramontano, Enzo; Costi, Roberta; Di Santo, Roberto - 01a Articolo in rivista
rivista: JOURNAL OF MEDICINAL CHEMISTRY (Washington, DC: American Chemical Society) pp. 8579-8598 - issn: 0022-2623 - wos: WOS:000668340800039 (9) - scopus: 2-s2.0-85108607601 (8)

11573/1553152 - 2021 - Anti-tumoral effects of a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative on head and neck squamous carcinoma cell lines
Nicolai, Alice; Madia, Valentina Noemi; Messore, Antonella; De Vita, Daniela; De Leo, Alessandro; Ialongo, Davide; Tudino, Valeria; Tortorella, Elisabetta; Scipione, Luigi; Taurone, Samanta; Pergolizzi, Tiziano; Artico, Marco; Di Santo, Roberto; Costi, Roberta; Scarpa, Susanna - 01a Articolo in rivista
rivista: PHARMACEUTICALS (Basel : MDPI, Molecular Diversity Preservation International, 2004-) pp. - - issn: 1424-8247 - wos: WOS:000666329400001 (6) - scopus: 2-s2.0-85110773299 (6)

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