Synthesis, structure and antitumor activity of a new water-soluble platinum complex, (1R,2R-cyclohexanediamine-N,N')[2-hydroxy-4-oxo-2-pentenoato(2-)-O2] platinum(II).
The reaction of dihydroxo(1R,2R-cyclohexanediamine)platinum(II) with 2,4-dioxopentanoic acid gave a water-soluble complex, (1R,2R-cyclohexanediamine-N,N')[2-hydroxy-4-oxo-2-pentenoato (2-)-O2] platinum(II). The structure of the complex was determined by X-ray crystal analysis. The data indicated a chelation of the acetylacetonato part of 2,4-dioxo-pentanoic acid to platinum(II). The complex showed moderate antitumor activity against murine leukemia L1210 in mice (T/C = 195% at a dose of 200 mg/kg) and high activity against cisplatin-resistant L1210 leukemia (T/C = 275% at a dose of 25 mg/kg).
Basic Research Laboratories, Toray Industries, Inc., Kanagawa, Japan.
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H
Kawai
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Kitano
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M
Mutoh
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Hata
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016190:Carboplatin / Q000494:pharmacology; D002945:Cisplatin / Q000494:pharmacology; D004351:Drug Resistance; D007939:Leukemia L1210 / Q000188:drug therapy*; D051379:Mice; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D014867:Water; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; D014867:Water; C081275:platinum(II) (1,2-cyclohexanediamine)(2-hydroxy-4-oxo-2-pentenoate); D016190:Carboplatin; D002945:Cisplatin