Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation

Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation

AbstractThe colchicine binding site of tubulin is a promising target for discovering novel antitumour agents. Previously, we identified 2-aryl-4-amide-quinoline derivatives displayed moderate tubulin polymerisation inhibitory activity and broad-spectrum in vitro antitumour activity. In this study, s...

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Bibliographic Details
Main Authors: Wei Liu, Youyou He, Zhongjie Guo, Miaomiao Wang, Xiaodong Han, Hairui Jia, Jin He, Shanshan Miao, Shengzheng Wang
Format: Article
Language:English
Published: Taylor & Francis Group 2023-12-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Tubulin inhibitors
colchicine binding site
structural optimisation
antitumour activity
Online Access:https://www.tandfonline.com/doi/10.1080/14756366.2022.2155815

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