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渥曼青霉素和去甲氧基维里丁荧光衍生物作为磷脂酰肌醇3激酶探针的合成

Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase.

作者信息

Giner José-Luis, Kehbein Karen A, Cook James A, Smith Michele C, Vlahos Chris J, Badwey John A

机构信息

Department of Chemistry, State University of New York-ESF, Syracuse, NY 13210, USA.

出版信息

Bioorg Med Chem Lett. 2006 May 1;16(9):2518-21. doi: 10.1016/j.bmcl.2006.01.091. Epub 2006 Feb 7.

DOI:10.1016/j.bmcl.2006.01.091
PMID:16464575
Abstract

Fluorescent analogs were synthesized of the potent PI 3-kinase inhibitors, wortmannin and demethoxyviridin. The esterification of 11-deacetylwortmannin, 17-hydroxywortmannin, and demethoxyviridin with the fluorescent carboxylic acids NBD-sarcosine and 7-dimethylaminocoumarin-4-acetic acid generated six novel fluorescent esters. Potent inhibition of PI 3-kinase-alpha was observed for the derivatives of 11-desacetylwortmannin and demethoxyviridin.

摘要

合成了强效PI 3-激酶抑制剂渥曼青霉素和去甲氧基维立定的荧光类似物。11-去乙酰渥曼青霉素、17-羟基渥曼青霉素和去甲氧基维立定与荧光羧酸NBD-肌氨酸和7-二甲基氨基香豆素-4-乙酸进行酯化反应，生成了六种新型荧光酯。观察到11-去乙酰渥曼青霉素和去甲氧基维立定的衍生物对PI 3-激酶α具有强效抑制作用。

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