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Title: Tuning the activity of platinum(IV) anticancer complexes through asymmetric acylation
Authors: Chin, C.F.
Tian, Q. 
Setyawati, M.I.
Fang, W. 
Tan, E.S.Q. 
Leong, D.T. 
Ang, W.H. 
Issue Date: 13-Sep-2012
Citation: Chin, 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.
Abstract: Platinum(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.
Source Title: Journal of Medicinal Chemistry
ISSN: 00222623
DOI: 10.1021/jm300580y
Appears in Collections:Staff Publications

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