Potential silicon-containing antifolates

被引：10
|
作者：
Taylor, EC [1 ]
Chaudhuri, RP
Watson, SE
机构：
[1] Princeton Univ, Dept Chem, Princeton, NJ 08544 USA
[2] Long Isl Univ, Dept Chem, Brooklyn, NY 11201 USA
来源：
TETRAHEDRON | 1999年 / 55卷 / 06期
关键词：
antitumor compounds; coupling reactions; enzyme inhibitors; silicon compounds;
D O I：
10.1016/S0040-4020(98)01207-1
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Novel silicon-containing folate derivatives were synthesized as potential inhibitors of folate-dependent enzymes in an attempt to develop more effective antitumor agents. A dimethylsilyl moiety was inserted into the sidechain of two known antifolates with the aim of improving passive transport properties and sidechain conformational flexibility. An efficient, convergent palladium-catalyzed coupling methodology was used to link known heterocycles to novel, highly functionalized vinyl and ethynyl silanes. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1631 / 1638
页数：8
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