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Giner JL, Kehbein KA, Cook
JA, Smith MC, Vlahos CJ, Badwey JA.
Synthesis of fluorescent derivatives of
wortmannin and demethoxyviridin as probes for
phosphatidylinositol 3-kinase.
Bioorg Med Chem Lett. 2006 May
1;16(9):2518-21.
Department of Chemistry, State University of New York-ESF,
Syracuse, NY 13210, USA. jlginer@syr.edu
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.
PMID: 16464575
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