Synthesis and biological evaluation of 5,6,7-trimethoxy- 1- benzylidene-3,4-dihydro-naphthalen-2-one as tubulinpolymerization inhibitors |
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Authors: | 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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Institution: | a School of Pharmacy, Second Military Medical University, Shanghai 200433, China;
b Department of Neonatology, Shanghai Children’s Hospital, Shanghai Jiao Tong University, Shanghai 200040, China;
c Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China |
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Abstract: | 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. |
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Keywords: | Tubulin polymerization inhibitor Antitumor agent Combretastatin-A4 analog |
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