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Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)
ISSN (Print): 1871-5206
ISSN (Online): 1875-5992
DOI: 10.2174/187152007779314017

Searching for the Magic Bullet: Anticancer Platinum Drugs Which Can Be Accumulated or Activated in the Tumor Tissue

Author(s): Markus Galanski and Bernhard K. Keppler
Pages 55-73 (19)
Cisplatin, carboplatin and oxaliplatin are anticancer drugs, which are efficiently used in the clinics all over the world. Besides a remarkable therapeutic efficacy in a series of solid tumors and outstanding activity of cisplatin against testicular germ-cell cancer, the platinum-based therapy is in part accompanied by a set of severe toxic side-effects. The design of platinum complexes being equipped with an exclusive selectivity for the tumoral tissue and exhibiting a lack of systemic toxicity (‘magic bullets’) is the great hope in the fight against cancer and also a motor within the expanding field of bioinorganic chemistry. In this review article, two promising strategies, namely accumulation and activation of tumor inhibiting platinum complexes specifically at the tumor site is presented, demonstrating a stepwise approach towards the ‘magic bullet’ concept propagated by Paul Ehrlich.
Platinum complexes, anticancer activity, mechanism of action, structure-activity relationships, synthesis, medicinal chemistry, accumulation, activation
Institute of Inorganic Chemistry,University of Vienna, Waehringer Strasse 42, A-1090 Vienna, Austria.