A New Platinum Anticancer Drug Forms a Highly Stereoselective Adduct with Duplex DNA

Yu Chen; John A Parkinson; Zijian Guo; Tom Brown; Peter J Sadler

doi:10.1002/(SICI)1521-3773(19990712)38:13/14<2060::AID-ANIE2060>3.0.CO;2-J

A New Platinum Anticancer Drug Forms a Highly Stereoselective Adduct with Duplex DNA

Angew Chem Int Ed Engl. 1999 Jul 12;38(13-14):2060-2063. doi: 10.1002/(SICI)1521-3773(19990712)38:13/14<2060::AID-ANIE2060>3.0.CO;2-J.

Authors

Yu Chen¹, John A Parkinson¹, Zijian Guo¹, Tom Brown², Peter J Sadler¹

Affiliations

¹ Department of Chemistry, University of Edinburgh, West Mains Road, Edinburgh EH9 3JJ (UK), Fax: (+44) 131-650-6452.
² Department of Chemistry, University of Southampton, Southampton SO17 1BJ (UK).

Abstract

The alignment of the 2-picoline ligand within the major groove contributes to the formation of a highly stereoselective GG intrastrand bischelate between the new anticancer drug cis-[PtCl₂(NH₃)(2-picoline)] and a 14-mer DNA duplex (see schematic representation).

Keywords: Antitumor agents; Bioinorganic chemistry; DNA recognition; Platinum; Stereoselectivity.