Bioorganic and Medicinal Chemistry Letters p. 2586 - 2590 (2010)
Update date:2022-08-05
Topics:
Bursavich, Matthew G.
Brooijmans, Natasja
Feldberg, Lawrence
Hollander, Irwin
Kim, Stephen
Lombardi, Sabrina
Park, Kaapjoo
Mallon, Robert
Gilbert, Adam M.
A series of benzofuran-3-one indole phosphatidylinositol-3-kinases (PI3K) inhibitors identified via HTS has been prepared. The optimized inhibitors possess single digit nanomolar activity against p110α (PI3K-α), good pharmaceutical properties, selectivity versus p110γ (PI3K-γ), and tunable selectivity versus the mammalian target of rapamycin (mTOR). Modeling of compounds 9 and 32 in homology models of PI3K-α and mTOR supports the proposed rationale for selectivity. Compounds show activity in multiple cellular proliferation assays with signaling through the PI3K pathway confirmed via phospho-Akt inhibition in PC-3 cells.
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