Synthesis and Antitumor Activity of Riboflavin and Flavin Mononucleotide Pt(II) Complexes

• Published in: Chemical & pharmaceutical bulletin Vol. 36; no. 5; pp. 1895 - 1898
• Main Authors: SUZUKI, KENJIRO, NOJI, MASAHIDE, TASHIRO, TAZUKO, KIDANI, YOSHINORI
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 1988; Maruzen; Japan Science and Technology Agency
• Subjects: 2-(aminomethyl)cyclohexylamine; Animals; Antineoplastic Agents - chemical synthesis; Chemistry; Coordination compounds; Cyclohexylamines - chemical synthesis; Cyclohexylamines - pharmacology; Exact sciences and technology; Inorganic chemistry and origins of life; Leukemia L1210 - drug therapy; Mice; Organoplatinum Compounds - chemical synthesis; Organoplatinum Compounds - pharmacology; Preparations and properties; Antineoplastic agent; Cationic complex; Divalent metal Complexes; Stereoisomer; Vitamin; Organic ligand; Platinum «II» Complexes; Ammino complex; Transition metal Complexes; Tricyclic compound; Biological activity; L1210 cell line; Diamine; Complexes Mixed; Preparation; Nucleotide; Aromatic compound
• DOI: 10.1248/cpb.36.1895
• ISSN: 0009-2363

Several Pt(II) complexes of riboflavin (RF) and flavin mononucleotide (FMN) with 1, 2-cyclohexanediamine (dach) or 2-(aminomethyl)cyclohexylamine (amcha) isomers were prepared. The coordination sites of RF or FMN to Pt(II) ions were determined to be N(5) and O(6) with resultant chelate ring formation.Antitumor activities of the dach or amcha Pt(II) complexes were tested against murine leukemia L1210 and all of them were antitumor-active. Pt(FMN)(trans-l-dach) exhibited the higher activity with a T/C% value of 326, with 4 cured mice out of 6. These results justify further testing.