Synthesis and Antitumor Activity of Pt (II) Complexes containing 2, 3-Diaminopropanol Isomers

• Published in: Chemical & pharmaceutical bulletin Vol. 31; no. 5; pp. 1469 - 1473
• Main Authors: NOJI, MASAHIDE, MOTOYAMA, SHIGERU, TASHIRO, TAZUKO, KIDANI, YOSHINORI
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 1983; Maruzen; Japan Science and Technology Agency
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Chemistry; conformation of chelate ring; Coordination compounds; Exact sciences and technology; Inorganic chemistry and origins of life; Leukemia L1210 - drug therapy; Mice; Platinum - pharmacology; Preparations and properties; Propanolamines - chemical synthesis; Propanolamines - pharmacology; Stereoisomerism; Antineoplastic agent; Structure effect; Divalent metal Complexes; Aminoalcohol; Preparation; Organic ligand; Platinoid Complexes; Transition metal Complexes; NMR spectrum; Biological activity; Platinum II Complexes
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.31.1469

Halogeno, sulfato, and nitrato Pt (II) complexes of 2, 3-diaminopropanol (pnOH) isomers were synthesized and their antitumor activities against leukemia L1210 were tested. The conformations of their chelate rings were determined to be λ-and δ-gauche forms for R- and S-pnOH, respectively, by 13C-nuclear magnetic resonance and circular dichroism spectral analyses. Among the pnOH isomers, Pt (II) complexes containing R-pnOH showed higher antitumor activity than those containing S- or racemic pnOH. It seems that there may be a relationship between the conformations of the chelate rings and antitumor activity in the case of five-membered chelate rings.