| Literature DB >> 21121631 |
Alban R Pereira1, Wendy K Strangman, Frederic Marion, Larry Feldberg, Deborah Roll, Robert Mallon, Irwin Hollander, Raymond J Andersen.
Abstract
Analogues of the sponge meroterpenoid liphagal have been synthesized and evaluated for inhibition of PI3Kα and PI3Kγ as part of a program aimed at developing new isoform-selective PI3K inhibitors. One of the analogues, compound 24, with IC₅₀ values of 66 nM against PI3Kα and 1840 nM against PI3Kγ, representing a 27-fold preference for PI3Kα, exhibited enhanced chemical stability and modestly enhanced potency and selectivity compared with the natural product liphagal.Entities:
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Year: 2010 PMID： 21121631 DOI： 10.1021/jm100531u
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446