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Curr Med Chem. 2019 Oct 3. doi: 10.2174/0929867326666191003154051. [Epub ahead of print]

Tubulin inhibitors binding to colchicine-site: A Review from 2015 to 2019.

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State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210023. China.
Neonatal Medical Center, Children's Hospital of Nanjing Medical University, Nanjing 210008, Jiangsu Province. China.


Based on three domains of colchicine-site which is conducive to the combination with small molecular compounds, colchicine-site on the tubulin has become a popular target for antitumor, that resulted in a great number of tubulin inhibitors binding to colchicine-site were reported and evaluated over the past years. Here, tubulin inhibitors targeting colchicine-site and their application to antitumor were reviewed from 2015 to 2019. Tubulin inhibitors were classified to ten categories according to structural features, as colchicine derivates, CA-4 analogues, chalcone analogues, coumarin analogs, indole hybrids, quinoline and quinazoline analogs, lignan and podophyllotoxin derivatives, phenothiazine analogs, N-heterocycle hybrids and others. Most of them possessing strong antitumor activity including antiproliferative potential against multi-drug-resistant (MDR) cell lines and anti-vascular properties both in vitro and in vivo. Therefore, in-depth analysis, lots of compounds were listed in tables as multi-target inhibitors, anti-MDR compounds, and inhibitors bearing antitumor activity in vivo. The latest research progress of tubulin inhibitors was demonstrated in this review, providing valuable reference and convenience for the research on tubulin inhibitors in future.


Antitumor activity; Colchicine-site; Multi-drug-resistance; Multi-target; Tubulin inhibitors

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