Hydroxamates: Relationships between Structure and Plasma Stability

被引：93
|
作者：
Flipo, Marion [1 ,3 ,4 ]
Charton, Julie [1 ,3 ,4 ]
Hocine, Akila [1 ,2 ,3 ,4 ]
Dassonneville, Sandrine [1 ,2 ,3 ,4 ]
Deprez, Benoit [1 ,2 ,3 ,4 ]
Deprez-Poulain, Rebecca [1 ,2 ,3 ,4 ]
机构：
[1] Univ Lille Nord France, INSERM, Biostruct & Drug Discovery U761, F-59006 Lille, France
[2] Univ Lille Nord France, Fac Pharm, F-59006 Lille, France
[3] Inst Pasteur, IFR 142, F-59021 Lille, France
[4] PRIM, F-59006 Lille, France
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 21期
关键词：
HISTONE DEACETYLASE INHIBITORS; MATRIX-METALLOPROTEINASE INHIBITORS; CONVERTING-ENZYME INHIBITORS; CANCER CELLS; POTENT; ACID; DISCOVERY; SERIES; DERIVATIVES; METABOLISM;
D O I：
10.1021/jm900648x
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Hydroxamates are valuable tools for chemical biology as well its interesting leads for medicinal chemistry. Although many hydroxamates display nanomolar activities against metalloproteases, only three hydroxamates have reached the market, among which is the HDAC inhibitor vorinostat. Failures in development are generally attributed to lack of selectivity, toxicity, or poor stability. To help medicinal chemists with respect to plasma stability, we have performed the first and preliminary study on structure-plasma stability for hydroxamates. We define some structural rules to predict or improve the plasma stability in the preclinical stage.
引用
收藏
页码：6790 / 6802
页数：13
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