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13 results on '"Gasparotto, V."'

11. Synthesis and in Vitro and in Vivo Antitumor Activity of 2-Phenylpyrroloquinolin-4-ones

Author

Ferlin, M. G., Chiarelotto, G., Gasparotto, V., Via, L. Dalla, Pezzi, V., Barzon, L., Palu, G., and Castagliuolo, I.

Abstract

In our search for potential new anticancer drugs, we designed and synthesized a series of tricyclic compounds containing the antimitotic 2-phenylazaflavone chromophore fused to a pyrrole ring in a pyrroloquinoline structure. Compounds 8, 18, 19, 22, 23, 25 and 26, when tested against a panel of fourteen human tumor cell lines, showed poor in vitro cytotoxic activity, whereas 20, 21 and 24 showed significant activity (IC50 0.7 to 50 μM). Steroid hormone-sensitive ovary, liver, breast and adrenal gland adenocarcinoma cell lines displayed the highest sensitivity (IC50 0.7 to 8 μM). Compound 24 blocked cells in the G2/M phase of the cell cycle and induced a significant increase in apoptotis. Compounds 20, 21 and 24 proved to alter microtubule assembly and stability, displaying a cytoplasmic microtubule network similar to that caused by Vincristine. In vivo, administration of compound 24 to Balb/c mice inhibited the growth of a syngenic hepatocellular carcinoma.

Published
2005

12. 3-substituted 7-phenyl-pyrroloquinolinones show potent cytotoxic activity in human cancer cell lines.

Author

Gasparotto V, Castagliuolo I, and Ferlin MG

Subjects
Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Cell Cycle drug effects, Cell Line, Tumor, Drug Resistance, Neoplasm, Drug Screening Assays, Antitumor, Flow Cytometry, Humans, Paclitaxel pharmacology, Pyrroles chemistry, Pyrroles pharmacology, Quinolones chemistry, Quinolones pharmacology, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Pyrroles chemical synthesis, Quinolones chemical synthesis
Abstract

A novel series of 3-alkyl-substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones (7-PPyQs) was synthesized with the aim to optimize the cytotoxic activity of recently identified PPyQs, promising inhibitors of tubulin polymerization. All compounds inhibited the growth of 11 human tumor cell lines at submicromolar concentrations as well as two human resistant cancer sublines, A549-T12 and A549-T24. FACS analysis indicated that all compounds caused significant arrest of the A549 cell cycle in G2/M phase at 0.1 and 1 muM and a good correlation between the cytotoxicity IC50 and their ability to block the cell cycle was observed.

Published
2007
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13. Synthesis and biological activity of 7-phenyl-6,9-dihydro-3H-pyrrolo[3,2-f]quinolin-9-ones: a new class of antimitotic agents devoid of aromatase activity.

Author

Gasparotto V, Castagliuolo I, Chiarelotto G, Pezzi V, Montanaro D, Brun P, Palù G, Viola G, and Ferlin MG

Subjects
Animals, Antimitotic Agents chemistry, Antimitotic Agents pharmacology, Biopolymers, Cell Line, Tumor, Cell Proliferation drug effects, Cytoskeleton drug effects, Drug Screening Assays, Antitumor, Flow Cytometry, Humans, Mice, Microscopy, Fluorescence, Neoplasm Transplantation, Pyrroles chemistry, Pyrroles pharmacology, Quinolones chemistry, Quinolones pharmacology, Structure-Activity Relationship, Transplantation, Isogeneic, Tritium, Tubulin chemistry, Water metabolism, Antimitotic Agents chemical synthesis, Aromatase metabolism, Pyrroles chemical synthesis, Quinolones chemical synthesis
Abstract

The newly synthesized 7-phenyl-3H-pyrrolo[3,2-f]quinolinones 16-26 and previously 27 and 28 were assayed for their in vitro antiproliferative activity on tumor cell lines, and the lead compound 16 in vivo on a singenic hepatocellular carcinoma in Balb/c mice. Results from FACS, immunofluorescence microscopy analysis, tubulin polymerization assay, and tritiated water release assay for the CYP19 activity confirmed the new compounds as potential anticancer agents acting by tubulin depolymerization, but devoid of aromatase activity unlike their geometric [2,3-h] isomers.

Published
2006
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