Hou, Wen; Lin, Hui; Wang, Zhen-Ya; Banwell, Martin; Zeng, Ting; Sun, Ping-Hua; Lin, Jing; Chen, Wei-Min
A series of novel bivalent securinine mimetics incorporating different linkers between C-15 and C-15′ were
synthesized and their topoisomerase I (Topo I) inhibitory activities evaluated. It was thus revealed that mimetic
R2 incorporating a rigid m-substituted benzene linker exhibits Topo I inhibitory activity three times
that of parent securinine. Comprehensive structure–activity relationship analyses in combination with
docking studies were used to rationalize the potent activity of these...[Show more]
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