Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils

被引：43

作者：

Hicks, Latorya D.

Hyatt, Janice L.

Moak, Teri

Edwards, Carol C.

Tsurkan, Lyudmila

Wierdl, Monika

Ferreira, Antonio M.

Wadkins, Randy M.

Potter, Philip M.

机构：

[1] St Jude Childrens Res Hosp, Dept Mol Pharmacol, Memphis, TN 38105 USA

[2] Univ Mississippi, Dept Chem & Biochem, University, MS 38677 USA

[3] St Jude Childrens Res Hosp, Hartwell Ctr Bioinformat & Biotechnol, Memphis, TN 38105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 11期

关键词：

fluorobenzil; fluorobenzoin; carboxylesterase; inhibitor;

D O I：

10.1016/j.bmc.2007.03.012

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：

We have synthesized and assessed the ability of symmetrical fluorobenzoins and fluorobenzils to inhibit mammalian carboxylesterases (CE). The majority of the latter were excellent inhibitors of CEs however unexpectedly, the fluorobenzoins were very good enzyme inhibitors. Positive correlations were seen with the charge on the hydroxyl carbon atom, the carbonyl oxygen, and the Hammett constants for the derived K-i values with the fluorobenzoins. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3801 / 3817

页数：17

共 34 条

[1] NEW LOOK AT STATISTICAL-MODEL IDENTIFICATION [J].