Synthesis of Novel gluco- and galacto-Functionalized Platinum Complexes

Abstract

Cisplatin, carboplatin, oxaliplatin and further derivatives are worldwide established cytostatics for the treatment of a vast range of tumours. These drugs showed extraordinary success; however, side effects and primary or developed secondary resistance of tumour cells represent severe problems, which prompt the development of novel functionalized platinum complexes. Selectively protected monohydroxy derivatives of glucose and galactose could be etherified by ?-halo ethers. Further, Finkelstein reaction and malonate synthesis gave precursor glycoconjugates which were easily transformed into their (diammine)platinum complexes. First tests with different tumour cell lines show biological activity of the gluco-functionalized platinum complex.(頗iley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)