Literature DB >> 16464575

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

José-Luis Giner1, Karen A Kehbein, James A Cook, Michele C Smith, Chris J Vlahos, John A Badwey.   

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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Year:  2006        PMID: 16464575     DOI: 10.1016/j.bmcl.2006.01.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Insights into the PI3-K-PKB-mTOR signalling pathway from small molecules.

Authors:  Richard M Gunn; Helen C Hailes
Journal:  J Chem Biol       Date:  2008-07-15

Review 2.  Optical molecular imaging and its emerging role in colorectal cancer.

Authors:  Rahul A Sheth; Umar Mahmood
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2010-07-01       Impact factor: 4.052

3.  Asterogynins: secondary metabolites from a Costa Rican endophytic fungus.

Authors:  Shugeng Cao; Leila Ross; Giselle Tamayo; Jon Clardy
Journal:  Org Lett       Date:  2010-10-15       Impact factor: 6.005

4.  A stabilized demethoxyviridin derivative inhibits PI3 kinase.

Authors:  Hushan Yuan; Monica T Pupo; Joe Blois; Adam Smith; Ralph Weissleder; Jon Clardy; Lee Josephson
Journal:  Bioorg Med Chem Lett       Date:  2009-05-30       Impact factor: 2.823

  4 in total

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