Natural products as lead structures: chemical transformations to create lead-like libraries

被引：71
|
作者：
Pascolutti, Mauro [1 ]
Quinn, Ronald J. [1 ]
机构：
[1] Griffith Univ, Eskitis Inst, Brisbane, Qld 4111, Australia
来源：
DRUG DISCOVERY TODAY | 2014年 / 19卷 / 03期
关键词：
DIVERSITY-ORIENTED SYNTHESIS; DRUG DISCOVERY; PARALLEL SYNTHESIS; COMBINATORIAL CHEMISTRY; BIOLOGICAL EVALUATION; SCREENING LIBRARIES; ORGANIC-SYNTHESIS; INHIBITORS; ANALOGS; DESIGN;
D O I：
10.1016/j.drudis.2013.10.013
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
In this review, we analyze and illustrate the variation of the two main lead-like descriptors [molecular weight (MW) and the partition coefficient (logP)] in the generation of libraries in which a natural product (NP) is used as the guiding structure. Despite the different approaches used to create NP-like libraries, controlling these descriptors during the synthetic process is important to generate lead-like libraries. From this analysis, we present a schematic approach to the generation of lead-like libraries that can be applied to any starting NP.
引用
收藏
页码：215 / 221
页数：7
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