| Title | Synthesis of Phosphatidylinositol 3-Kinase (PI3K) Inhibitory Analogues of the Sponge Meroterpenoid Liphagal. |
| Publication Type | Journal Article |
| Year of Publication | 2010 |
| Authors | Pereira, AR, Strangman, WK, Marion, F, Feldberg, L, Roll, D, Mallon, R, Hollander, I, Andersen, RJ |
| Journal | Journal of Medicinal Chemistry |
| Volume | 53 |
| Pagination | 8523 - 8533 |
| Date Published | 2010/// |
| ISBN Number | 0022-2623 |
| Keywords | liphagal 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)] |
