Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors
Abstract Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors using a parallel-synthesis approach led to the identification of a novel 4′,5-bisthiazole sub-series. The synthesis and optimisation of both the affinity pocket and (S)-proline amide moieties within this 4′,5-bisthiazole sub-series are described. From this work a number of analogues, including 14 (A66) and 24, were identified as potent and selective PI3Kα inhibitor in vitro tool compounds.
Fairhurst, Robin A.,Imbach-Weese, Patricia,Gerspacher, Marc,Caravatti, Giorgio,Furet, Pascal,Zoller, Thomas,Fritsch, Christine,Haasen, Dorothea,Trappe, Joerg,Guthy, Daniel A.,Arz, Dorothee,Wirth, Jasmin
p. 3569 - 3574
(2015/08/06)
ORGANIC COMPOUNDS
The resent invention relates to a com ound of formula (I) and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-
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Page/Page column 52
(2009/07/25)
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