期刊
BIOORGANIC CHEMISTRY
卷 93, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.103319
关键词
Resveratrol-cinnamoyl derivates; Tubulin polymerization inhibitors; Colchicine binding site; Anti-proliferative
资金
- National Natural Science Foundation of China [81602985, 81703754]
- Fundamental Research Funds for the Central Universities [2632018ZD19, 2632018ZD18]
- Natural Science Foundation of Jiangsu Province [BK20160763]
- Program for Chang jiang Scholars and Innovative Research Team in University [IRT_15R63]
- 111 Project from Ministry of Education of China
- State Administration of Foreign Export Affairs of China [B18056]
- Double First-Class University Project [CPU2018GF03]
A novel series of resveratrol-cinnamoyl hybrids as tubulin polymerization inhibitors were designed and synthesized, and evaluated for their anti-proliferative activities against A549, MCF-7, HepG2, HeLa and MDA-MB231 five cancer cell lines. Most designed compounds showed better anti-proliferative activities. Particularly, compound 6h exhibited the potent anti-proliferative activities with the IC50 value of 0.12, 0.016, 0.44, 0.37 and 0.78 mu M against A549, MCF-7, HepG2, HeLa and MDA-231, respectively, which was superior to that of reference drug colchicine. Besides, compound 6h displayed a remarkable inhibition of tubulin polymerization and a great potency to compete with [H-3] colchicine in binding to tubulin. Further studies indicated that compound 6h could induce the MCF-7 cells arrest in the G2/M phase. What' more, compound 6h induced cell apoptosis in a dose-dependent manner, and regulated the expression level of apoptosis-related proteins. These results revealed that compound 6h is a promising tubulin polymerization inhibitor for treatment of cancer and it is worthy of further exploitation.
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