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

页码：1631 / 1638

页数：8

共 18 条

[1]

BALDWIN SW, 1992, J MED CHEM, V35, P4450

[2] TOTAL SYNTHESIS OF 6-SILASTEROID RING-SYSTEM [J].