CONFORMATIONALLY CONSTRAINED ANALOGS OF DIACYLGLYCEROL .6. CHANGES IN PK-C BINDING-AFFINITY FOR 3-O-ACYL-2-DEOXY-L-RIBONOLACTONES BEARING DIFFERENT ACYL CHAINS

被引：15

作者：

MARQUEZ, VE ^{[1
]}

LEE, JW ^{[1
]}

SHARMA, R ^{[1
]}

TENG, K ^{[1
]}

WANG, SM ^{[1
]}

LEWIN, NE ^{[1
]}

BAHADOR, A ^{[1
]}

KAZANIETZ, MG ^{[1
]}

BLUMBERG, PM ^{[1
]}

机构：

[1] NCI,CELLULAR CARCINOGENESIS & TUMOR PROMOT LAB,BETHESDA,MD 20892

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)80144-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several 3-O-acyl-2-deoxy-L-ribonolactones with various acyl chains were synthesized and evaluated for their ability to compete with [H-3]phorbol-12,13-dibutyrate in a PK-C binding assay. A parabolic correlation between log 1/K-i and log water solubility [log (WS)] revealed the importance of branching of the acyl chain as a means to increase affinity. As in the case of the diacylglycerols, this effect possibly is related to the de-stabilization of the lipid bilayer induced by the presence of a ''kink'' in the modified acyl chains.

引用

页码：355 / 360

页数：6

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