On May 15, 2017, Song, Anran; Zhang, Jianbin; Ge, Yang; Wang, Changyuan; Meng, Qiang; Tang, Zeyao; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Computed Properties of 16230-24-3 The title of the article was C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRT790M mutant. And the article contained the following:
With the aim to overcome the drug resistance induced by the EGFR T790M mutation (EGFRT790M), herein, a family of diphenylpyrimidine derivatives (Sty-DPPYs) bearing a C-2 (E)-4-(styryl)aniline functionality were designed and synthesized as potential EGFRT790M inhibitors. Among them, the compound 10e (N-[3-[[5-fluoro-2-[(E)-4-(3,5-dimethylstyryl)phenylamino]-4-pyrimidinyl]amino]phenyl]-2-acrylamide) displayed strong potency against the EGFRT790M enzyme, with the IC50 of 11.0 nM. Compound 10e also showed a higher SI value (SI = 49.0) than rociletinib (SI = 21.4), indicating its less side effect. In addition, compound 10e could effectively inhibit the proliferation of H1975 cells harboring the EGFRT790M mutation, within the concentration of 2.91 μM. Significantly, compound 10e has low toxicity against the normal HBE cell (IC50 = 22.48 μM). This work provided new insights into the discovery of potent and selective inhibitor against EGFRT790M over wild-type (EGFRWT). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Computed Properties of 16230-24-3
The Article related to styrylaniline diphenylpyrimidine derivative preparation egfr mutant kinase inhibitor, nonsmall cell lung carcinoma antitumor resistance diphenylpyrimidine derivative egf, diphenylpyrimidine, egfr(t790m), inhibitor, nsclc, resistance and other aspects.Computed Properties of 16230-24-3
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