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

• 作 者: 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
• 机 构: School of Pharmacy,Second Military Medical University,Shanghai Institute of Pharmaceutical Industry,
• 出 处: Chinese Chemical Letters
• 发表日期: 2015年05期
• 关键词: polymerization tubulin analogs linking substituted membered bioactivity assembly

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 lb with amino substituted on position 3 of B ring conferred optimal bioactivity,higher than that of the lead compound 22 b 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.

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 as.These compounds appear to be potential tubulin-polymerization inhibitors .Compounds lb with amino substituted on position 3 of B ring conferred optimal bioactivity, higher than that of lead compound 22 b 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 provide a new structural type for the development of novel antitumor agents.