Novel bivalent securinine mimetics as topoisomerase I inhibitors
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|
|Source:||Med. Chem. Commun.|
|Hou W et al Novel bivalent securinine 2017.pdf||1.26 MB||Adobe PDF|
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