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ChemInform Abstract: Synthesis and in vitro Evaluation of New Wortmannin Esters: Potent Inhibitors of Phosphatidylinositol 3-Kinase.

✍ Scribed by L. C. CREEMER; H. A. KIRST; C. J. VLAHOS; R. M. SCHULTZ

Publisher
John Wiley and Sons
Year
2010
Weight
29 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

title esters, e.g. (Ib)-(Ie), are synthesized by deacetylation and subsequent reacylation of wortmannin (Ia). In comparison with the latter one, they show superior inhibition of phosphatidylinositol (PI) 3-kinase and increased cell cytotoxicity in vitro. Reduction of (Ib) to (IIa) slightly enhances activity while further acetylation to (IIb) leads to a dramatic loss in activity. These new esters are good candidates to explore the in vivo antitumor effects of PI 3-kinase inhibitors. -

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