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À propos de : Synthesis and in Vitro Evaluation of New Wortmannin Esters: PotentInhibitors of Phosphatidylinositol 3-Kinase        

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  • Synthesis and in Vitro Evaluation of New Wortmannin Esters: PotentInhibitors of Phosphatidylinositol 3-Kinase
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  • New C-11 esters of the fermentation product wortmannin have beensynthesized, with someof them further derivatized at C-17. The new esters show greaterinhibition of isolatedphosphatidylinositol 3-kinase and increased cell cytotoxicity in arapidly proliferating leukemiacell line, when compared to wortmannin. Reduction of the C-17ketone caused a slight increasein activity, while acylation of this new alcohol caused severe loss ofactivity. With theirincreased activity, the new C-11 esters may be good candidates toexplore the in vivo antitumoreffects of phosphatidylinositol 3-kinase inhibitors.
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