{"id":9750,"date":"2022-09-15T03:37:04","date_gmt":"2022-09-14T19:37:04","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9750"},"modified":"2022-09-15T03:37:04","modified_gmt":"2022-09-14T19:37:04","slug":"long-yi-team-published-research-on-european-journal-of-medicinal-chemistry-in-2021-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9750","title":{"rendered":"Long, Yi team published research on European Journal of Medicinal Chemistry  in 2021 | 761446-44-0"},"content":{"rendered":"<p>Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is  1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.  Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. <a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">COA of Formula: C10H17BN2O2<\/a>.<\/p>\n<p>Yu, Mingfeng;Long, Yi;Yang, Yuchao;Li, Manjun;Teo, Theodosia;Noll, Benjamin;Philip, Stephen;Wang, Shudong research published \u300a Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation\u300b, the research content is summarized as follows. CDK8 is deregulated in multiple types of human cancer and is viewed as a therapeutic target for the treatment of the disease. Accordingly, the search for small-mol. inhibitors of CDK8 is being intensified. Capitalising on our initial discovery of AU1-100, a potent CDK8 inhibitor yet with a limited degree of kinase selectivity, a structure-based optimization was carried out, with a series of new multi-substituted pyridines rationally designed, chem. prepared and biol. evaluated. Such endeavour has culminated in the identification of 42, a more potent CDK8 inhibitor with superior kinomic selectivity and oral bioavailability. The mechanism underlying the anti-proliferative effect of 42 on MV4-11 cells was studied, revealing that the compound arrested the G1 cell cycle and triggered apoptosis. The low risk of hepato- and cardio-toxicity of 42 was estimated These findings merit further investigation of 42 as a targeted cancer therapeutic.<\/p>\n<p><a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">COA of Formula: C10H17BN2O2<\/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\">COA of Formula: C10H17BN2O2<\/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-9750","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>Long, Yi team published research on European Journal of Medicinal Chemistry in 2021 | 761446-44-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. COA of Formula: C10H17BN2O2.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=9750\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Long, Yi team published research on European Journal of Medicinal Chemistry in 2021 | 761446-44-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. 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