An orally active antitumor cyclohexanediamine-Pt(IV) complex: trans,cis,cis-bis(n-valerato)(oxalato)(1R,2R-cyclohexane diamine)Pt(IV).

Abstract

In order to develop orally active antitumor platinum complexes, several cyclohexanediamine-Pt(IV) complexes of a general formula trans,cis,cis-[Pt(IV) (OCOCnHn+1)2 (oxalato)(1R,2R-cyclohexanediamine)] were synthesized by derivatizing oxaliplatin [Pt(II)(oxalato)(1R,2R-cyclohexanediamine), I-OHP], which is a potent antitumor cyclohexanediamine-Pt(II) complex we have prepared and now undergoing clinical trials. The I-OHP derivatives were found to be stable, lipophilic and reduced to yield I-OHP, an active species, quantitatively by ascorbate in vitro. All the derivatives were antitumor active against mouse lymphocytic leukemia L1210 when given i.p. In particular, trans-bis-valerato-oxalato-1R,2R-dach-Pt(IV), C5-OHP, showed markedly high activity. C5-OHP also exhibited significant antitumor activity against L1210 when orally administered. C5-OHP was considered to be a suitable candidate for the oral cancer chemotherapy agent to be developed.

• Authors: R Kizu, T Nakanishi, M Miyazaki, T Tashiro, M Noji, A Matsuzawa, M Eriguchi, Y Takeda, N Akiyama, Y Kidani
• Journal: Anti-cancer drugs (Anticancer Drugs) Vol. 7 Issue 3 Pg. 248-56 (May 1996) ISSN: 0959-4973 [Print] England
• PMID: 8791997 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antineoplastic Agents
• Organoplatinum Compounds
• bis-valerato-oxalato-1,2-diaminocyclohexaneplatinum
• Ascorbic Acid

Topics

• Animals
• Antineoplastic Agents (pharmacology)
• Ascorbic Acid
• Chromatography, High Pressure Liquid
• Drug Stability
• Leukemia L1210 (drug therapy)
• Mice
• Organoplatinum Compounds (pharmacology)
• Solubility
• Tumor Cells, Cultured