title: Synthesis, structure, and antitumor activity of 1,3-dithiol- and 1,3-dithiolan-2-ylidenemalonatoplatinum(II) complexes.
abstract: 1,3-Dithiol- and 1,3-dithiolan-2-ylidenemalonatoplatinum(II) complexes A2Pt(OOC)2C = CR2 (A = NH3, cyclopropylamine (CPA) or A2 = ethylenediamine(EDA), trans(+/-)-1,2-diaminocyclohexane(DACH); R2 = -SCH = CHS-, -SCH2CH2S-) have been synthesized and subjected to in vivo assay for antitumor activity after characterization by means of elemental analysis, IR spectroscopy, and x-ray analysis. The molecular structure of (CPA)2Pt(OOC)2C = CSCH = CHS has been determined by x-ray diffraction: space group P2(1)/n, a = 7.955(1), b = 16.912(2), c = 15.116(2) A, beta = 102.74(1) degrees, z = 4, R = 0.032, Rw = 0.035. Among the Pt(II) complexes studied, biscyclopropylamineplatinum(II) complexes both of the above-mentioned dicarboxylate leaving groups exhibited much higher antitumor activity against the leukemia L1210 cell line compared with the known cisplatin.
authors.affiliation: Korea Institute of Science & Technology, Seoul.
authors.forename: Y S
authors.initials: YS
authors.lastname: Sohn
authors.forename: K M
authors.initials: KM
authors.lastname: Kim
authors.forename: J H
authors.initials: JH
authors.lastname: Jeong
authors.forename: D Y
authors.initials: DY
authors.lastname: Noh
authors.forename: C O
authors.initials: CO
authors.lastname: Lee
authors.forename: S U
authors.initials: SU
authors.lastname: Choi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D018360:Crystallography, X-Ray; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C087099:platinum(II) bis(cyclopropylamine)-1,3-dithiol-2-ylidenemalonate