Abstract
A series of 1,3,6-triphenylpyrazolo[3,4-b]pyridin-4-one derivatives was designed, synthesized and evaluated for cytotoxic activity in A375 human melanoma and human erythroleukemia (HEL) cells. The new pyrazolopyridones displayed comparable activities to the antitumor compound etoposide. The inhibitory effect of compounds 17, 18, 27 and 32 against topoisomerase II-mediated cleavage activities was measured finding good correlation with the results obtained from MTS assay. Docking studies into bacterial topoisomerase II (DNA Gyrase), topoisomerase IIα and topoisomerase IIβ binding sites in the DNA binding interface were performed.
Keywords: Pyrazolo[3, 4-b]pyridine, etoposide, topoisomerase, docking studies.
Medicinal Chemistry
Title:Synthesis and Biological Evaluation of Pyrazolo[3,4-b]pyridin-4-ones as a New Class of Topoisomerase II Inhibitors
Volume: 11 Issue: 4
Author(s): Mojgan Aghazadeh Tabrizi, Pier Giovanni Baraldi, Stefania Baraldi, Filippo Prencipe, Delia Preti, Giulia Saponaro, Romeo Romagnoli, Stefania Gessi, Stefania Merighi, Angela Stefanelli, Debora Fazzi, Pier Andrea Borea, Rodolfo Couto Maia, Nelilma C. Romeiro, Carlos A. M. Fraga and Eliezer J. Barreiro
Affiliation:
Keywords: Pyrazolo[3, 4-b]pyridine, etoposide, topoisomerase, docking studies.
Abstract: A series of 1,3,6-triphenylpyrazolo[3,4-b]pyridin-4-one derivatives was designed, synthesized and evaluated for cytotoxic activity in A375 human melanoma and human erythroleukemia (HEL) cells. The new pyrazolopyridones displayed comparable activities to the antitumor compound etoposide. The inhibitory effect of compounds 17, 18, 27 and 32 against topoisomerase II-mediated cleavage activities was measured finding good correlation with the results obtained from MTS assay. Docking studies into bacterial topoisomerase II (DNA Gyrase), topoisomerase IIα and topoisomerase IIβ binding sites in the DNA binding interface were performed.
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Tabrizi Aghazadeh Mojgan, Baraldi Giovanni Pier, Baraldi Stefania, Prencipe Filippo, Preti Delia, Saponaro Giulia, Romagnoli Romeo, Gessi Stefania, Merighi Stefania, Stefanelli Angela, Fazzi Debora, Borea Andrea Pier, Maia Couto Rodolfo, Romeiro C. Nelilma, Fraga A. M. Carlos and Barreiro J. Eliezer, Synthesis and Biological Evaluation of Pyrazolo[3,4-b]pyridin-4-ones as a New Class of Topoisomerase II Inhibitors, Medicinal Chemistry 2015; 11 (4) . https://dx.doi.org/10.2174/1573406411666141210141317
DOI https://dx.doi.org/10.2174/1573406411666141210141317 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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