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

Lei Zhao ,  Jiu-Jiu Zhou ,  Xin-Ying Huang ,  Li-Ping Cheng ,  Wan Pang ,  Zhen-Peng Kai ,  Fan-Hong Wu

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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

    • 通讯作者: Wan Pang,
    Zhen-Peng Kai,
    Fan-Hong Wu,
  • 基金项目:

    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)

摘要: 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.

English

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  • 发布日期:  2015-05-12
  • 收稿日期:  2015-02-25
  • 网络出版日期:  2015-04-27
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