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Design, synthesis, and biological evaluation of diaryl heterocyclic derivatives targeting tubulin polymerization with potent anticancer activities. 2023
Gang Li, and
Jia-Qiang Wu, and
Xiaojia Cai, and
Wen Guan, and
Zhijun Zeng, and
Yanghui Ou, and
Xiaoyun Wu, and
Jiayu Li, and
Xiangxiang Fang, and
Jinling Liu, and
Yali Zhang, and
Huamin Wang, and
Canqiang Yin, and
Hongliang Yao
Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, 510260, China.
A series of diaryl heterocyclic analogues were designed and synthesized as tubulin polymerization inhibitors. Among them, compound 6y showed the highest antiproliferative activity against HCT-116 colon cancer cell line with an IC50 values of 2.65 μM. Compound 6y also effectively inhibited tubulin polymerization in vitro (IC50 of 10.9 μM), and induced HCT-116 cell cycle arrest in G2/M phase. In addition, compound 6y exhibited high metabolic stability on human liver microsomes (T1/2 = 106.2 min). Finally, 6y was also effective in suppressing tumor growth in a HCT-116 mouse colon model without apparent toxicity. Collectively, these results suggest that 6y represents a new class of tubulin inhibitors deserving further investigation.
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