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Synthesis and biological evaluation of 5,6,7-trimethoxy- 1- benzylidene-3,4-dihydro-naphthalen-2-one as tubulinpolymerization inhibitors

Jun-Hang Jiang ,  Can-Hui Zheng ,  Chong-Qing Wang ,  Juan Wang ,  Wei Tian ,  Chao Yang ,  Yun-Long Song ,  Yong Hu ,  Ju Zhu ,  You-Yun Zhou

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Citation:  Jun-Hang Jiang, Can-Hui Zheng, Chong-Qing Wang, Juan Wang, Wei Tian, Chao Yang, Yun-Long Song, Yong Hu, Ju Zhu, You-Yun Zhou. Synthesis and biological evaluation of 5,6,7-trimethoxy- 1- benzylidene-3,4-dihydro-naphthalen-2-one as tubulinpolymerization inhibitors[J]. Chinese Chemical Letters, 2015, 26(5): 607-609. doi: 10.1016/j.cclet.2015.03.022 shu

Synthesis and biological evaluation of 5,6,7-trimethoxy- 1- benzylidene-3,4-dihydro-naphthalen-2-one as tubulinpolymerization inhibitors

    • 通讯作者: Yong Hu,
    Ju Zhu,
    You-Yun Zhou,
  • 基金项目:

    Shanghai Natural Science Foundation (No. 09ZR1438800)  (No. 09ZR1438800)

    Shanghai Education Development Foundation (No. 12CG42). (No. 12CG42)

摘要: A series of new combretastatin-A4 analogs were synthesized, in which a six-membered ring connects the linking bridge and A ring, and their tumor cell growth and tubulin-polymerization inhibitory activity were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 1b with amino substituted on position 3 of B ring conferred optimal bioactivity, higher than that of the lead compound 22b and equivalent to that of CA-4. The binding modes of these compounds to tubulin were obtained by molecular docking, which can explain the structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.

English

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  • 发布日期:  2015-03-27
  • 收稿日期:  2015-01-18
  • 网络出版日期:  2015-02-28
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