{"id":10778,"date":"2022-10-28T06:39:16","date_gmt":"2022-10-27T22:39:16","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10778"},"modified":"2022-10-28T06:39:16","modified_gmt":"2022-10-27T22:39:16","slug":"zhang-lingzhi-team-published-research-in-molecules-in-2020-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10778","title":{"rendered":"Zhang, Lingzhi team published research in Molecules  in 2020 | 761446-44-0"},"content":{"rendered":"<p>Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is  1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.   1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. <a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">SDS of cas: 761446-44-0<\/a>.<\/p>\n<p>Zhang, Lingzhi;Ju, Qiurong;Sun, Jinjin;Huang, Lei;Wu, Shiqi;Wang, Shuping;Li, Yin;Guan, Zhe;Zhu, Qihua;Xu, Yungen research published \u300a Discovery of novel dual extracellular regulated protein kinases (ERK) and phosphoinositide 3-kinase (PI3K) inhibitors as a promising strategy for cancer therapy\u300b, the research content is summarized as follows. The scaffold-hopping generation of a series of 1H-pyrazolo[3,4-d]pyrimidines <strong>I<\/strong> (R<sup>1<\/sup> = 2-methylpyridin-4-yl, 1-methyl-1H-pyrazol-4-yl; R<sup>2<\/sup> = Bn, cyclopentyl) dual ERK\/PI3K inhibitors was reported. 1-(7-(1H-Pyrazol-4-yl)pyrido[3,2-d]pyrimidin-2-yl)-3-cyclopentylurea was the most promising candidate, with potent inhibitory activities against both ERK2 and PI3K\u03b1 which displays superior anti-proliferative profiles against HCT116 and HEC1B cancer cells. Meanwhile, 1-(7-(1H-pyrazol-4-yl)pyrido[3,2-d]pyrimidin-2-yl)-3-cyclopentylurea possessed acceptable pharmacokinetic profiles and showed more efficacious anti-tumor activity than GDDC-0980 and the corresponding drug combination (BVD-523 + GDDC-0980) in HCT-116 xenograft model, with a tumor growth inhibitory rate of 51% without causing observable toxic effects. All the results indicated that 1-(7-(1H-pyrazol-4-yl)pyrido[3,2-d]pyrimidin-2-yl)-3-cyclopentylurea was a highly effective anticancer compound and provided a promising basis for further optimization towards dual ERK\/PI3K inhibitors.<\/p>\n<p><a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">SDS of cas: 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p><a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">SDS of cas: 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[733,131],"tags":[716],"class_list":["post-10778","post","type-post","status-publish","format-standard","hentry","category-761446-44-0","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Zhang, Lingzhi team published research in Molecules in 2020 | 761446-44-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. 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