Antitumor and DNA-binding properties of a group of oligomeric complexes of platinum(II) and platinum(IV)
- 1 August 1990
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 33 (8) , 2184-2188
- https://doi.org/10.1021/jm00170a022
Abstract
The antitumor and DNA-binding properties of a group of oligomeric platinum (II) and platinum (IV) complexes are described. The compounds, having the stoichiometry [cis-PtII(X)2(.mu.-OH)]2 (NO3)2, where X is NH3, NH2CH2CH3, and NH2CH(CH3)2, were found to be inactive or only weakly active against L-1210 leukemia. In vitro studies involving PM2-DNA show that these compounds bind to and unwind closed circular DNA in a manner similar to cis-PtII-(NH3)2Cl2. The Pt(IV) complexes produced by hydrogen peroxide oxidation of the Pt(II) dimers are inactive as antitumor agents and are incapable of unwinding PM2-DNA. The cyclotrimer [cis-PtII(RR-DACH)(.mu.-OH)]3(NO3)3, where RR-DACH is (R,R)-1,2 diaminocyclohexane, exhibits potent antitumor activity against L-1210 leukemia and modest activities with B-16 and M5076 tumor lines. This compound platinates DNA, causing DNA unwinding and mobility shifts.This publication has 3 references indexed in Scilit:
- INTRACELLULAR BIOTRANSFORMATION OF PLATINUM COMPOUNDS WITH THE 1,2-DIAMINOCYCLOHEXANE CARRIER LIGAND IN THE L1210 CELL-LINE1988
- Comparative antitumor studies on platinum(II) and platinum(IV) complexes containing 1,2-diaminocyclohexaneJournal of Medicinal Chemistry, 1987
- Binding ofcis- andtrans-Dichlorodiammineplatinum(II) to DNA: Evidence for Unwinding and Shortening of the Double HelixScience, 1979