{"id":10691,"date":"2022-10-27T02:54:57","date_gmt":"2022-10-26T18:54:57","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10691"},"modified":"2022-10-27T02:54:57","modified_gmt":"2022-10-26T18:54:57","slug":"tong-lexian-team-published-research-in-european-journal-of-medicinal-chemistry-in-2019-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10691","title":{"rendered":"Tong, Lexian team published research in European Journal of Medicinal Chemistry  in 2019 | 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\">Electric Literature of 761446-44-0<\/a>.<\/p>\n<p>Tong, Lexian;Song, Pinrao;Jiang, Kailong;Xu, Lei;Jin, Tingting;Wang, Peipei;Hu, Xiaobei;Fang, Sui;Gao, Anhui;Zhou, Yubo;Liu, Tao;Li, Jia;Hu, Yongzhou research published \u300a Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies\u300b, the research content is summarized as follows. Through virtual screening, we identified the lead compound MCL1020, which exhibited modest CHK1 inhibitory activity. Then a series of 5-(pyrimidin-2-ylamino)picolinonitrile derivatives as CHK1 inhibitors were discovered by further rational optimization. One promising mol., <strong>I<\/strong>, whose potency was one of the best, had an IC<sub>50<\/sub> of 0.4 nM with remarkable selectivity (&gt;4300-fold CHK1 vs. CHK2). Compound <strong>I<\/strong> effectively inhibited the growth of malignant hematopathy cell lines especially Z-138 (IC<sub>50<\/sub>: 0.013 \u03bcM) and displayed low affinity for hERG (IC<sub>50<\/sub> &gt; 40 \u03bcM). Moreover, <strong>I<\/strong> significantly suppressed the tumor growth in Z-138 cell inoculated xenograft model (20 mg\/kg I.V., TGI = 90.29%) as a single agent with body weight unaffected. Taken together, our data demonstrated compound <strong>I<\/strong> could be a promising drug candidate for the treatment of hematol. malignancies.<\/p>\n<p><a href=\"https:\/\/www.ambeed.com\/products\/761446-44-0.html\">Electric Literature of 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\">Electric Literature of 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-10691","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>Tong, Lexian team published research in European Journal of Medicinal Chemistry in 2019 | 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. Electric Literature of 761446-44-0.\" \/>\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=10691\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Tong, Lexian team published research in European Journal of Medicinal Chemistry in 2019 | 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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