1. Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase
- Author
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Michele C. Smith, John A. Badwey, José-Luis Giner, Karen A Kehbein, James A. Cook, and Chris J. Vlahos
- Subjects
Stereochemistry ,Clinical Biochemistry ,Molecular Conformation ,Molecular Probe Techniques ,Pharmaceutical Science ,Phosphatidylinositol 3-Kinases ,Biochemistry ,Chemical synthesis ,Wortmannin ,Structure-Activity Relationship ,chemistry.chemical_compound ,Drug Discovery ,Structure–activity relationship ,Phosphatidylinositol ,Enzyme Inhibitors ,Molecular Biology ,Fluorescent Dyes ,Phosphoinositide-3 Kinase Inhibitors ,chemistry.chemical_classification ,biology ,Organic Chemistry ,Stereoisomerism ,Fluorescence ,Androstadienes ,chemistry ,Enzyme inhibitor ,biology.protein ,Molecular Medicine ,Androstenes ,Lactone - 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.
- Published
- 2006
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