Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.
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Pereira AR, Strangman WK, Marion F, Feldberg L, Roll D, Mallon R, Hollander I, Andersen RJ
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. Epub 2010 Dec 1.
- PubMed ID
- 21121631 [ View in PubMed]
- Abstract
Analogues of the sponge meroterpenoid liphagal have been synthesized and evaluated for inhibition of PI3Kalpha and PI3Kgamma as part of a program aimed at developing new isoform-selective PI3K inhibitors. One of the analogues, compound 24, with IC(5)(0) values of 66 nM against PI3Kalpha and 1840 nM against PI3Kgamma, representing a 27-fold preference for PI3Kalpha, exhibited enhanced chemical stability and modestly enhanced potency and selectivity compared with the natural product liphagal.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Wortmannin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform IC 50 (nM) 12 N/A N/A Details