3,4,5-三取代2(5H)-呋喃酮组合文库的合成。第一部分:卤代5-烷氧基-2(5H)-呋喃酮子库的构建。

Drug design and discovery Pub Date : 1999-11-01
E Lattmann, D C Billington, C A Langley
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引用次数: 0

摘要

从糠醛开始,5-羟基-3,4-二卤-2(5H)-呋喃酮和5-羟基-4氯-2(5H)-呋喃酮转化为3个卤化的5-烷氧基-2(5H)-呋喃酮亚库。通过选择4种胺,对24种卤代5-烷氧基2(5H)-呋喃酮的反应活性进行了化学评价。伪黏液卤素酯的生物学评价结果发现了一种具有有效抗癌活性的先导结构。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of combinatorial libraries of 3,4,5-trisubstituted 2(5H)-furanones. Part One: Construction of a sub-library of halogenated 5-alkoxy-2(5H)-furanones.

Starting from furfural, 5-hydroxy-3,4-dihalo-2(5H)-furanones and 5-hydroxy-4 chloro-2(5H)-furanone were converted into 3 sublibraries of halogenated 5-alkoxy-2(5H)-furanones. The reactivity of 24 halogenated 5-alkoxy2(5H)-furanones was chemically evaluated by using 4 selected amines for subsequent reactions. The biological evaluation of the pseudo-muco halogen esters resulted in the discovery of a lead structure with potent anti-cancer activity.

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