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

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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. Epub 2006 Feb 7.

PubMed ID

16464575 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Wortmannin	Phosphatidylinositol 3-kinase regulatory subunit alpha	IC 50 (nM)	1.2	N/A	N/A	Details