Organoplatinum antitumor agents have had tremendous effectiveness against various forms of cancer. The discovery of cis-dichlorodiamineplatinum(II) (Cisplatin), the first of the organoplatinum antitumor drugs represented a major advance in the treatment of this disease. The early drugs were platinum(II) compounds containing two cis inert ligands and two labile ligands (necessary for hydrolysis and subsequent binding to adjacent guanine units of DNA). Three of these compounds (Cisplatin, Oxaloplatin and Carboplatin) are currently commercial successes widely used in cancer treatment. However, administration of these drugs is accompanied by rather severe side effects such as kidney damage and nausea due to low water solubility and dose-limiting side-effects. A way to address this problem is to deliver the drug at low concentration such that the antitumor activity is maintained while the threshold for toxicity is not reached. To provide a release vehicles, platinum(II) end-capped glycerol adipic acid hyperbranched polyesters were prepared. The materials not only contain releasable platinum moieties as an integral part of the structure but also provide a water-soluble carrier.

Platinum(II) end-capped glycerol/adipic acid poly(ester)s as antitumor prodrugs

255th National Meeting (2018)

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