Tritiated platinum antitumor agents containing the trans-(d,1)-1,2-diaminocyclohexane carrier ligand
✍ Scribed by Steven D. Wyrick; Stephen G. Chaney
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 365 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Cis-diamminedichloroplatinum (11) (cisplatin) is one of the most widely used anticancer drugs today. However, platinum compounds possessing the 1,2-diaminocyclohexane (DACH) carrier ligand offer advantages over cisplatin with regard to bioavailability, activity and decreased renal toxicity. diaminocyclohexane derivatives are the isomeric forms recently chosen by the NCI for large animal studies and phase 1/11 clinical trials. Here we report the synthesis of four trans-(d,l)-1.2diaminocyclo-hexane platinum derivatives labeled with tritium in the cyclohexane ring by catalytic reduction of a cyclohexene precursor with carrier-free tritium gas over 10% Pd/C.