HIGHLY-ACTIVE ANTITUMOR PLATINUM(II) COMPLEXES OF AMINO-SUGARS

被引:54
作者
TSUBOMURA, T [1 ]
OGAWA, M [1 ]
YANO, S [1 ]
KOBAYASHI, K [1 ]
SAKURAI, T [1 ]
YOSHIKAWA, S [1 ]
机构
[1] UNIV TOKYO,FAC ENGN,DEPT SYNTHET CHEM,TOKYO 113,JAPAN
关键词
D O I
10.1021/ic00339a019
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The syntheses, structures, spectroscopic properties, and antitumor activities of a series of platinum(II) diamino sugar complexes, [PtCl2(diamino sugar)], have been studied. The molecular structure of one of these is described. Crystal data for [PtCl2(Me-ManNN)]·H2O (Me-ManNN = methyl 2,3-diamino-2,3-dideoxy-α-D-mannopyranoside) are as follows: C7H]8N2O5Cl2Pt; fw = 476.2 monoclinic, P21, a = 10.048 (2) Å, b = 8.725 (2) Å, c = 7.584 (2) Å, β = 90.67 (2)°, V= 664.8 (3) Å3, Dc = 2.39 g cm-3, Z)0 = 2.37 g cm’3, 2=2, and μ = 110.8 cm1 (Mo Kα). Antitumor activity was investigated against SI80 and LI210 tumors. In the SI80 study, the life span of mice treated with [PtCl2(GlcNN)]-H20 (GlcNN = 2,3-diamino-2,3-dideoxy-D-glucose) increased, and the T/C value was up to 410%. Other compounds also showed high activities (T/C = 200-380%) against S180. The correlation between the chelate conformation of diamino sugar ligands and the antitumor activity is discussed. © 1990, American Chemical Society. All rights reserved.
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页码:2622 / 2626
页数:5
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