2. Academic Validation
  3. Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal

Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal

  • J Med Chem. 2010 Dec 23;53(24):8523-33. doi: 10.1021/jm100531u.
Alban R Pereira 1,  Wendy K Strangman,  Frederic Marion,  Larry Feldberg,  Deborah Roll,  Robert Mallon,  Irwin Hollander,  Raymond J Andersen
Affiliations

Affiliation

  • 1 Department of Chemistry, University of British Columbia, Vancouver, British Columbia, Canada.
PMID: 21121631 DOI: 10.1021/jm100531u
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.

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