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Title: Harnessing chemoselective imine ligation for tethering bioactive molecules to platinum(iv) prodrugs
Authors: Wong, D.Y.Q.
Lau, J.Y.
Ang, W.H. 
Issue Date: 28-May-2012
Citation: Wong, D.Y.Q., Lau, J.Y., Ang, W.H. (2012-05-28). Harnessing chemoselective imine ligation for tethering bioactive molecules to platinum(iv) prodrugs. Dalton Transactions 41 (20) : 6104-6111. ScholarBank@NUS Repository.
Abstract: Platinum(ii) anticancer drugs are among the most effective and often used chemotherapeutic drugs. In recent years, there has been increasing interest in exploiting inert platinum(iv) scaffolds as a prodrug strategy to mitigate the limitations of platinum(ii) anticancer complexes. In this prodrug strategy, the axial ligands are released concomitantly upon intracellular reduction to the active platinum(ii) congener, offering the possibility of conjugating bioactive co-drugs which may synergistically enhance cytotoxicity on cancer cells. Existing techniques of tethering bioactive molecules to the axial positions of platinum(iv) prodrugs suffer from limited scope, poor yields and low reliability. This report explores the applications of current chemoselective ligation chemistries to platinum(iv) anticancer complexes with the aim of addressing the aforementioned limitations. Here, we describe the synthesis of a platinum(iv) complex bearing an aromatic aldehyde functionality and explored the scope of imine ligation with various hydrazide and aminooxy functionalized substrates. As a proof of concept, we tethered a six sequence long peptide mimetic (AMVSEF) of the anti-inflammatory protein, ANXA1. © 2012 The Royal Society of Chemistry.
Source Title: Dalton Transactions
ISSN: 14779226
DOI: 10.1039/c2dt30264k
Appears in Collections:Staff Publications

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