On January 31, 2020, Miao, Xiuqi; Xing, Lingyun; Guo, Ming; Zhang, Hong; Liu, Sicong; Yin, Shiliang; Gong, Ping; Zhang, Dajun; Zhai, Xin published an article.Application In Synthesis of 2-Chloroacetamide The title of the article was Design, synthesis and biological evaluation of 2-arylaminopyrimidine derivatives bearing 1,3,8-triazaspiro[4,5]decan-4-one or piperidine-3-carboxamide moiety as novel Type-I1/2 ALK inhibitors. And the article contained the following:
Aiming to develop novel Type-I1/2 inhibitors of ALK to overcome extensive resistance mutations, especially the L1196M mutation surrounding the ATP pocket, two series of 2-arylaminopyrimidine derivatives (I (R1 = pyrrolidin-1-yl, piperidin-1-yl, 4-methylpiperazin-1-yl, 4-(2-hydroxyethyl)piperazin-1-yl), II (R2 = 4-methylpiperazin-1-yl, 4-(2-hydroxyethyl)piperazin-1-yl) and III (R3 = ethoxycarbonylmethylamino, 2-(piperidin-1-yl)acetamido, 2-(4-methylpiperazin-1-yl)acetamido, etc.), IV (R4 = allyl, cyclopropanecarbonyl, 2-carboxyethyl, etc.)) were designed based on scaffold hopping. The extensive structural elaboration discovered compound IV ((A), R4 = 3-ethoxy-3-oxopropyl) which possessed excellent IC50 values of 0.06 and 0.23μM against ALK-pos. Karpas299 and H2228 cell lines, resp. Meanwhile, (A) displayed encouraging inhibitory potency in the ALKWT (2.5 nM) and ALKL1196M (6.5 nM) enzymic assays. Furthermore, the AO/EB and Hoechst 33258 assays illustrated that (A) could induce cell apoptosis in a dose-dependent manner. Eventually, the mol. docking of (A) with ALK clearly presented the vital interactions within the active site, which was in accordance with Type-I1/2 inhibitor binding mode. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application In Synthesis of 2-Chloroacetamide
The Article related to arylaminopyrimidine triazaspirodecanone preparation alk inhibitor antitumor docking, piperidine carboxamide arylaminopyrimidine preparation alk inhibitor antitumor docking, imidazolidin-2-one, l1196m mutants, piperidine-3-carboxamide, type-i(1/2) alk inhibitor and other aspects.Application In Synthesis of 2-Chloroacetamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics