Ontology highlight
ABSTRACT:
SUBMITTER: Liu W
PROVIDER: S-EPMC9848350 | biostudies-literature | 2023 Dec
REPOSITORIES: biostudies-literature
Liu Wei W He Youyou Y Guo Zhongjie Z Wang Miaomiao M Han Xiaodong X Jia Hairui H He Jin J Miao Shanshan S Wang Shengzheng S
Journal of enzyme inhibition and medicinal chemistry 20231201 1
The 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 <i>in vitro</i> antitumour activity. In this study, structure based rational design and systematic structural optimisation were performed to obtain analogues <b>C1∼J2</b> bearing diverse substituents and scaffolds. Among them, analogue <b>G13</b> bearing ...[more]