Conformationally constrained analogues of diacylglycerol (DAG).: 14.: Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement

被引：20

作者：

Marquez, VE ^{[1
]}

Sharma, R

Wang, SM

Lewin, NE

Blumberg, PM

Kim, IS

Lee, J

机构：

[1] NCI, Med Chem Lab, NIH, Bethesda, MD 20892 USA

[2] NCI, Lab Cellular Carcinogenesis & Tumor Promot, Div Basic Sci, NIH, Bethesda, MD 20892 USA

[3] Seoul Natl Univ, Med Chem Lab, Coll Pharm, Kwanak Ku, Seoul 151742, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 13期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/S0960-894X(98)00307-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The replacement of the sn-l and sn-2 carbonyl esters in DAG-surrogate lactones by sulfonate esters showed that their isosteric properties in protein kinase C binding are controlled by the location of the hydrophobic alkyl chain on the molecule. The CO and SO2 groups appear to be true isosteres only when they are adjacent to the alkyl chain, which is presumed to insert normal to the lipid bilayer. Published by Elsevier Science Ltd.

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收藏

页码：1757 / 1762

页数：6

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