Synthesis, structure, and antitumor activity of 1,3-dithiol- and 1,3-dithiolan-2-ylidenemalonatoplatinum(II) complexes.
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.
Sohn
Y S
YS
Korea Institute of Science & Technology, Seoul.
Kim
K M
KM
Jeong
J H
JH
Noh
D Y
DY
Lee
C O
CO
Choi
S U
SU
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
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C087099:platinum(II) bis(cyclopropylamine)-1,3-dithiol-2-ylidenemalonate