Design, synthesis and biological evaluation of 3,4-dihydronaphthalen-1(2H)-one derivatives as Bcl-2 inhibitors

作者：Wang, Fuli; Zhang, Rongxiang; Cui, Yong; Sheng, Liping; Sun, Yinping; Tian, Wei; Liu, Xiao; Liang, Shuzeng^*

来源：Research on Chemical Intermediates, 2017, 43(10): 5933-5942.

DOI：10.1007/s11164-017-2972-x

• Anticancer activity
• Cytotoxicity
• Bcl-2 inhibitors

A series of new 3,4-dihydronaphthalen-1(2H)-one derivatives (6a-f) were designed, and synthesized by the Claisen-Schmidt condensation reaction. Their structures were characterized by NMR, FTIR, and MS spectroscopy. Their antitumor activities against human neoplastic cell lines Hela, Hepg2, K562, THP-1, SW1990, MIA PaCa-2, NCI-H460 and SK-BR-3 by the MTT method exhibited obvious anticancer activities and their cytotoxicities for LO2 cell lines were lower than DOX, especially for 6b and 6d. The inhibition activities against the Bcl-2 protein for 6b was evaluated and the result shows that lipophilic 3,4-dimethoxybenzylidene and 3,4-dihydronaphthalen-1(2H)-one could bind slightly to the active pockets of the Bcl-2 protein. @@@ [GRAPHICS]

• 出版日期2017-10
• 单位山东大学; 山东省千佛山医院