{"id":10102,"date":"2022-10-14T07:45:02","date_gmt":"2022-10-13T23:45:02","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102"},"modified":"2022-10-14T07:45:02","modified_gmt":"2022-10-13T23:45:02","slug":"bin-huachaos-team-published-research-in-european-journal-of-medicinal-chemistry-in-2022-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102","title":{"rendered":"Bin, Huachao&#8217;s team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0"},"content":{"rendered":"<p>In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.<a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">COA of Formula: C10H17BN2O2<\/a> The author mentioned the following in the article:<\/p>\n<p>Ataxia telangiectasia mutated and Rad3-related (ATR) kinase is an important regulator of the DNA damage response (DDR), especially in response to replication stress (RS). Tumor cells with ataxia-telangiectasia mutated (ATM) kinase loss of function or DDR defects that promote replicative stress are often more reliant on ATR for survival, highlighting ATR as a good antitumor target under the principle of synthetic lethality. Herein we report the discovery of a potent and highly selective ATR inhibitor, SKLB-197, which was obtained through structural optimization and structure-activity relationship (SAR) studies towards a hit compound (Cpd-1). SKLB-197 showed an IC50 value of 0.013 \u03bcM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo. In addition, this compound exhibited good pharmacokinetic properties. Overall, SKLB-197 could be a promising lead compound for drug discovery targeting ATR and deserves further in-depth studies. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0<a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">COA of Formula: C10H17BN2O2<\/a>)<\/p>\n<p>1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory,  antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">COA of Formula: C10H17BN2O2<\/a><\/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>1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory,  antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">COA of Formula: C10H17BN2O2<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[744,131],"tags":[129],"class_list":["post-10102","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Bin, Huachao&#039;s team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.COA of Formula: C10H17BN2O2 The author mentioned the following in the article:\" \/>\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=10102\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Bin, Huachao&#039;s team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.COA of Formula: C10H17BN2O2 The author mentioned the following in the article:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-13T23:45:02+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102\",\"name\":\"Bin, Huachao's team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-13T23:45:02+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.COA of Formula: C10H17BN2O2 The author mentioned the following in the article:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10102#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Bin, Huachao&#8217;s team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. 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The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.COA of Formula: C10H17BN2O2 The author mentioned the following in the article:","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102","og_locale":"en_US","og_type":"article","og_title":"Bin, Huachao's team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0 | pyrazoles-derivatives","og_description":"In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aDiscovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo\u300b.COA of Formula: C10H17BN2O2 The author mentioned the following in the article:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-10-13T23:45:02+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"2 minutes"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=10102","name":"Bin, Huachao's team published research in European Journal of Medicinal Chemistry in 2022 | CAS: 847818-74-0 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-10-13T23:45:02+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"In 2022,Bin, Huachao; Chen, Pei; Wu, Ming; Wang, Falu; Lin, Guifeng; Pan, Shulei; Liu, Jingming; Mu, Bo; Nan, Jinshan; Huang, Qiao; Li, Linli; Yang, Shengyong published an article in European Journal of Medicinal Chemistry. 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