On December 15, 2020, Teng, Yu; Li, Xinyu; Ren, Shengnan; Cheng, Yu; Xi, Kun; Shen, Hongtao; Ma, Wenzhuo; Luo, Guoshun; Xiang, Hua published an article.Quality Control of N-(3-Aminophenyl)acrylamide The title of the article was Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. And the article contained the following:
Herein, a series of quinazoline derivatives I [R1 = Br, 3-pyridyl, (6-fluoro-3-pyridyl), (6-chloro-3-pyridyl), 3-quinolyl; R2 = vinyl, Et, HC=CH2CH3, C≡CCH3; R3 = H, Me] bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me]. Compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, compoundI [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] could be identified as a promising PI3Kδ inhibitor worthy of further profiling. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide
The Article related to quinazoline preparation pi3k delta inhibitor docking human, bromoquinazolinyl amino phenyl boric acid suzuki coupling catalyst palladium, boric acid bromoquinazolinyl oxy phenyl suzuki coupling catalyst palladium, quinolineboronic acid bromoquinazolinyl amino phenyl suzuki coupling catalyst palladium, b-cell malignancies, pi3kδ, quinazoline derivatives and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics