期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 55, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2021.116597
关键词
Anticancer; Indole derivatives; Microtubules; Tubulin polymerization inhibitors; Colchicine binding site
资金
- National Natural Science Foundation of China [21877087, 22074114, 21971043, 81861138046]
- Natural Science Foundation of Hubei Province, China [2021CFB556, 2020CFB623]
- Science and Technology Commission of Shanghai Municipality [17XD1404400, 18XD1400800, 19ZR1403400]
- Key Laboratory for Green Chemical Process of Ministry of Education [GCP20200201]
- Hubei Key Laboratory of Novel Reactor and Green Chemical Technology [40201002]
- Wuhan Institute of Technology Teaching Research Project [X2017034]
This review summarizes the recent progress in the development of indole derivatives as tubulin polymerization inhibitors from 2010 to present. It provides useful clues and inspirations for the further design of outstanding inhibitors.
The alpha-and beta-tubulins are the major polypeptide components of microtubules (MTs), which are attractive targets for anticancer drug development. Indole derivatives display a variety of biological activities including antitumor activity. In recent years, a great number of indole derivatives as tubulin polymerization inhibitors have sprung up, which encourages medicinal chemists to pursue promising inhibitors with improved antitumor activities, excellent physicochemical, pharmacokinetic and pharmacodynamic properties. In this review, the recent progress from 2010 to present in the development of indole derivatives as tubulin polymerization inhibitors was summarized and reviewed, which would provide useful clues and inspirations for further design of outstanding tubulin polymerization inhibitors.
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