Strategies for the synthesis of novel indole alkaloid-based screening libraries for drug discovery

被引：22

作者：

Fokas, Demosthenes ^{[1
]}

Yu, Libing ^{[1
]}

Baldino, Carmen M. ^{[1
]}

机构：

[1] ArQule Inc, Dept Chem, Woburn, MA 01801 USA

来源：

MOLECULAR DIVERSITY | 2005年 / 9卷 / 1-3期

关键词：

diversity oriented synthesis; indolazonines; polycyclic indolic compounds; skeletal diversity; solution-phase chemistry; beta-tetrahydrocarbolines;

D O I：

10.1007/s11030-005-1292-z

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of diverse indole-based chemotypes were synthesized from beta-tetrahydrocarboline (beta-THC) scaffolds prepared from commercially and readily available tryptamines and alpha-ketoesters. Diversity can be generated within these chemotypes through the following strategies: (a) appendage of substituents to the beta-THC scaffold, prepared in situ or as a template, through further elaboration and (b) skeletal modifications to the beta-THC scaffold via ring forming or ring breaking reactions. The strategies described here are amenable to high throughput solution-phase parallel synthesis, providing access to novel indole-based screening libraries for drug discovery.

引用

页码：81 / 89

页数：9

共 44 条

[1] Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT(2B)) contractile receptor in the rat stomach fundus [J].