Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase
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DOI：
10.1016/j.bmcl.2006.01.091
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发表时间：
2006-05-01
影响因子：
2.7
通讯作者：
Badwey, JA
中科院分区：
文献类型：
--
作者：
Giner, JL;Kehbein, KA;Badwey, JA
合成了有效的PI 3-激酶抑制剂渥曼青霉素和脱甲氧基绿啶的荧光类似物。11-脱乙酰渥曼青霉素、17-羟基渥曼青霉素和脱甲氧基绿啶分别与荧光羧酸NBD-肌氨酸和7-二甲氨基香豆素-4-乙酸酯化，生成6种新型荧光酯。观察到11-脱乙酰渥曼青霉素和脱甲氧基绿啶的衍生物对PI 3-激酶-α的有效抑制。(C)2006爱思唯尔有限公司保留所有权利。
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. (C) 2006 Elsevier Ltd. All rights reserved.