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Synthesis of Phosphatidylinositol 3-Kinase (PI3K) Inhibitory Analogues of the Sponge Meroterpenoid Liphagal.

TitleSynthesis of Phosphatidylinositol 3-Kinase (PI3K) Inhibitory Analogues of the Sponge Meroterpenoid Liphagal.
Publication TypeJournal Article
Year of Publication2010
AuthorsPereira, AR, Strangman, WK, Marion, F, Feldberg, L, Roll, D, Mallon, R, Hollander, I, Andersen, RJ
JournalJournal of Medicinal Chemistry
Volume53
Pagination8523 - 8533
Date Published2010///
ISBN Number0022-2623
Keywordsliphagal stereoselective racemic nonracemic analog prepn phosphatidylinositol kinase inhibition, structure liphagal analog inhibition selectivity phosphatidylinositol kinase alpha gamma
Abstract

The sponge meroterpenoid liphagal (+)-I and racemic and nonracemic analogs such as (±)-II were prepd. and their inhibition of phosphatidylinositol-3-kinases α and γ (PI3Kα and PI3Kγ, resp.) was detd. II inhibited PI3Kα and PI3Kγ with IC50 values of 66 nM and 1840 nM, resp., showing a 27-fold preference for PI3Kα; in addn., II exhibited enhanced chem. stability and modestly enhanced potency and selectivity compared with those of I. [on SciFinder(R)]