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Novel bivalent securinine mimetics as topoisomerase I inhibitors

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dc.contributor.authorHou, Wen
dc.contributor.authorLin, Hui
dc.contributor.authorWang, Zhen-Ya
dc.contributor.authorBanwell, Martin
dc.contributor.authorZeng, Ting
dc.contributor.authorSun, Ping-Hua
dc.contributor.authorLin, Jing
dc.contributor.authorChen, Wei-Min
dc.date.accessioned2017-04-04T00:45:41Z
dc.date.available2017-04-04T00:45:41Z
dc.date.issued2017-02
dc.description.abstractA 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 bivalent mimetics. Mechanistic studies served to confirm the deductions arising from docking studies that the active bivalent mimetics not only inhibited complexation between Topo I and DNA but also stabilized the Topo I–DNA complex itself.en_AU
dc.description.sponsorshipThis work was supported by the National Natural Science Foundation of China (Grant No. 81273362).en_AU
dc.format10 pagesen_AU
dc.format.mimetypeapplication/pdfen_AU
dc.identifier.issn2040-2503en_AU
dc.identifier.urihttp://hdl.handle.net/1885/114379
dc.publisherRoyal Society of Chemistryen_AU
dc.rightsThis article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material.en_AU
dc.sourceMed. Chem. Commun.en_AU
dc.subjectnovelen_AU
dc.subjectbivalenten_AU
dc.subjectsecurinineen_AU
dc.subjectmimeticsen_AU
dc.subjectlinkersen_AU
dc.subjectC-15en_AU
dc.subjectC-15′en_AU
dc.subjecttopoisomerase I (Topo I)en_AU
dc.subjectinhibitoryen_AU
dc.subjectactivitiesen_AU
dc.subjectR2en_AU
dc.titleNovel bivalent securinine mimetics as topoisomerase I inhibitorsen_AU
dc.typeJournal articleen_AU
dcterms.accessRightsOpen Accessen_AU
dcterms.dateAccepted2016-12-23
local.bibliographicCitation.issue2en_AU
local.bibliographicCitation.lastpage328en_AU
local.bibliographicCitation.startpage320en_AU
local.contributor.affiliationBanwell, Martin G., RSC General, CPMS Research School of Chemistry, The Australian National Universityen_AU
local.contributor.authoruidu9500594en_AU
local.identifier.citationvolume8en_AU
local.identifier.doi10.1039/C6MD00563Ben_AU
local.identifier.essn2040-2511en_AU
local.publisher.urlhttp://www.rsc.org/en_AU
local.type.statusPublished Versionen_AU

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