Citation: Lei Zhao, Jiu-Jiu Zhou, Xin-Ying Huang, Li-Ping Cheng, Wan Pang, Zhen-Peng Kai, Fan-Hong Wu. Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs[J]. Chinese Chemical Letters, ;2015, 26(8): 993-999. doi: 10.1016/j.cclet.2015.05.003 shu

Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs

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School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, China

Corresponding author: Wan Pang, Zhen-Peng Kai, Fan-Hong Wu,
Received Date: 25 February 2015
Available Online: 27 April 2015
Fund Project: This work was supported by the National Natural Science Foundation of China (Nos. 21472126, 21402122) (Nos. 21472126, 21402122)Shanghai Municipal Natural Science Foundation (No. 12ZR450200). (No. 12ZR450200)

A total of 11 novel combretastatin A-4 (CA-4) analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes: (i) hydrogenated derivatives, (ii) ethoxyl derivatives, (iii) amino derivatives and (iv) pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure-activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.
- Combretastatin A-4,
- Anti-proliferative,
- Synthesized
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沈阳化工大学材料科学与工程学院沈阳 110142