Optimization of cisplatin for the treatment of hormone dependent tumoral diseases Part 1: Use of steroidal ligands

Platinum complexes such as cisplatin and carboplatin are metal based drugs, which are widely used in cancer chemotherapy. However, in the current therapy of hormone-dependent breast and prostate cancer they are not established. This might be the result of intrinsic and acquired resistance of the tumors during the therapy. Therefore, several attempts were done to design platinum complexes to address these tumors. Steroidal and non-steroidal drugs were modified for the coordination to platinum. The mode of action implies a binding to the estrogen receptor, a selective accumulation in the tumor cells and a specific binding to DNA. In part 1 of this review article we describe the use of steroidal ligands to optimize cisplatin for the treatment of hormone dependent tumoral diseases. (C) 2009 Elsevier B.V. All rights reserved.