Cisplatin: Synthesis, antitumour activity and mechanism of action

Abstract

A review is presented on the successful antitumour drug cis-diamminedichloroplatinum(II), better known as cisplatin. Special attention is given to the synthesis of the compound and related derivatives, and to the nature of the hydrolysis products in blood and in the cell. In the second part of the review the mechanism of action is discussed. Binding to DNA and in particular the formation of intrastrand cross-links between adjacent guanines, to which the Pt(NH3)2(2+) ion is chelated at the N7 atoms, seems to be a very important event. However, at the moment it is not yet known which DNA lesion is responsible for the killing of the tumour cells.