Novel bivalent securinine mimetics as topoisomerase I inhibitors
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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]
Collections | ANU Research Publications |
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Date published: | 2017-02 |
Type: | Journal article |
URI: | http://hdl.handle.net/1885/114379 |
Source: | Med. Chem. Commun. |
DOI: | 10.1039/C6MD00563B |
Access Rights: | Open Access |
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File | Description | Size | Format | Image |
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Hou W et al Novel bivalent securinine 2017.pdf | 1.26 MB | Adobe PDF | ![]() |
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