73286-71-2, Name is N-Boc-2-pyrroline, belongs to pyrrolines compound, is a common compound. SDS of cas: 73286-71-2In an article, once mentioned the new application about 73286-71-2.
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kbeta/delta inhibitors for the treatment of PTEN-deficient tumours
Attempts to lock the active conformation of compound 4, a PI3Kbeta/delta inhibitor (PI3Kbeta cell IC50 0.015?muM), led to the discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-ones, which showed high levels of potency and selectivity as PI3Kbeta/delta inhibitors. Compound 10 proved exquisitely potent and selective: PI3Kbeta cell IC50 0.0011?muM in PTEN null MDA-MB-468 cell and PI3Kdelta cell IC50 0.014?muM in Jeko-1 B-cell, and exhibited suitable physical properties for oral administration. In vivo, compound 10 showed profound pharmacodynamic modulation of AKT phosphorylation in a mouse PTEN-null PC3 prostate tumour xenograft after a single oral dose and gave excellent tumour growth inhibition in the same model after chronic oral dosing. Based on these results, compound 10 was selected as one of our PI3Kbeta/delta preclinical candidates.
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Reference£º
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem