Hu, Shengquan published the artcileDesign, synthesis and biological evaluation of 4-aryl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one derivatives as a PI3Kα inhibitor, Quality Control of 1197171-76-8, the publication is Biological & Pharmaceutical Bulletin (2019), 42(6), 1013-1018, database is CAplus and MEDLINE.
A series of 4-aryl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one derivatives I [R = Ph, 6-amino-3-pyridyl, 2-amino-1,3-benzoxazol-5-yl, etc.] were designed as a phosphoinositide 3-kinase α (PI3Kα) inhibitor by scaffold hopping. The target compounds I were synthesized from di-Et malonate and Et chloroacetate by nucleophilic substitution, ring-closure, chlorination and Suzuki reaction, etc. The biol. activities of compounds I were evaluated with cytotoxic activity in vitro on Uppsala 87 Malignant Glioma (U87MG) and prostate cancer-3 (PC-3) by cell counting kit-8 (CCK-8). The results showed that compound I [R = 6-amino-3-pyridyl] displayed higher inhibition than pos. control PI-103, and high PI3Kα inhibitory activity with IC50 of 113 ± 9nM in same order of magnitude as BEZ235. In addition, the LogKow values and mol. docking studies were performed to further investigate drug-like properties of target compounds I and interactions between compound I [R = 6-amino-3-pyridyl] and PI3Kα.
Biological & Pharmaceutical Bulletin published new progress about 1197171-76-8. 1197171-76-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is N-Methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, and the molecular formula is C14H20BNO3, Quality Control of 1197171-76-8.
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