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Novel bivalent securinine mimetics as topoisomerase I inhibitors

Hou, Wen; Lin, Hui; Wang, Zhen-Ya; Banwell, Martin; Zeng, Ting; Sun, Ping-Hua; Lin, Jing; Chen, Wei-Min

Description

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]

CollectionsANU Research Publications
Date published: 2017-02
Type: Journal article
URI: http://hdl.handle.net/1885/114379
Source: Med. Chem. Commun.
DOI: 10.1039/C6MD00563B

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