Please use this identifier to cite or link to this item: https://doi.org/10.1021/jm300580y
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dc.titleTuning the activity of platinum(IV) anticancer complexes through asymmetric acylation
dc.contributor.authorChin, C.F.
dc.contributor.authorTian, Q.
dc.contributor.authorSetyawati, M.I.
dc.contributor.authorFang, W.
dc.contributor.authorTan, E.S.Q.
dc.contributor.authorLeong, D.T.
dc.contributor.authorAng, W.H.
dc.date.accessioned2014-06-17T07:50:57Z
dc.date.available2014-06-17T07:50:57Z
dc.date.issued2012-09-13
dc.identifier.citationChin, C.F., Tian, Q., Setyawati, M.I., Fang, W., Tan, E.S.Q., Leong, D.T., Ang, W.H. (2012-09-13). Tuning the activity of platinum(IV) anticancer complexes through asymmetric acylation. Journal of Medicinal Chemistry 55 (17) : 7571-7582. ScholarBank@NUS Repository. https://doi.org/10.1021/jm300580y
dc.identifier.issn00222623
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/64757
dc.description.abstractPlatinum(II) anticancer drug cisplatin is one of the most important chemotherapeutic agents in clinical use but is limited by its high toxicity and severe side effects. Platinum(IV) anticancer prodrugs can overcome these limitations by resisting premature aquation and binding to essential plasma proteins. Structure-activity relationship studies revealed a link between the efficacy of platinum(IV) complexes with the nature of their axial ligands, which can be modified to enhance the properties of the prodrug. The existing paradigm of employing platinum(IV) complexes with symmetrical axial carboxylate ligands does not fully exploit their vast potential. A new approach was conceived to control properties of platinum(IV) prodrugs using contrasting axial ligands via sequential acylation. We report a novel class of asymmetric platinum(IV) carboxylates based on the cisplatin template containing both hydrophilic and lipophilic ligands on the same scaffold designed to improve their aqueous properties and enhance their efficacy against cancer cells in vitro. © 2012 American Chemical Society.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1021/jm300580y
dc.sourceScopus
dc.typeArticle
dc.contributor.departmentCHEMICAL & BIOMOLECULAR ENGINEERING
dc.contributor.departmentCHEMISTRY
dc.description.doi10.1021/jm300580y
dc.description.sourcetitleJournal of Medicinal Chemistry
dc.description.volume55
dc.description.issue17
dc.description.page7571-7582
dc.description.codenJMCMA
dc.identifier.isiut000308675800020
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