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

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

José-Luis Giner  1 , Karen A Kehbein, James A Cook, Michele C Smith, Chris J Vlahos, John A Badwey
Affiliations

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

José-Luis Giner et al. Bioorg Med Chem Lett. .

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.

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