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Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase
Journal article   Peer reviewed

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

José-Luis Giner, Karen A Kehbein, James A. Cook, Michele C. Smith, Chris J. Vlahos and John A. Badwey
Bioorganic & medicinal chemistry letters, Vol.16(9), pp.2518-2521
2006
DOI: https://doi.org/10.1016/j.bmcl.2006.01.091
PMID: 16464575

Abstract

Enzyme inhibitors Fluorescent probes Phosphoinositol 3-kinase Steroidal drugs
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-α was observed for the derivatives of 11-desacetylwortmannin and demethoxyviridin.

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