{"id":12168,"date":"2023-02-07T02:27:13","date_gmt":"2023-02-06T18:27:13","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12168"},"modified":"2023-02-07T02:27:13","modified_gmt":"2023-02-06T18:27:13","slug":"johannes-jeffrey-w-et-al-published-their-research-in-acs-medicinal-chemistry-letters-in-2015-cas-18213-75-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12168","title":{"rendered":"Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7"},"content":{"rendered":"<p>Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. Ann;Casella, Robert;Croft, Rosemary A.;Dishington, Allan P.;Gingipalli, Lakshmaiah;Gu, Chungang;Hawkins, Janet L.;Holmes, Jane L.;Howard, Tina;Huang, Jian;Ioannidis, Stephanos;Kazmirski, Steven;Lamb, Michelle L.;McGuire, Thomas M.;Moore, Jane E.;Ogg, Derek;Patel, Anil;Pike, Kurt G.;Pontz, Timothy;Robb, Graeme R.;Su, Nancy;Wang, Haiyun;Wu, Xiaoyun;Zhang, Hai-Jun;Zhang, Yue;Zheng, Xiaolan;Wang, Tao. And the article was included in ACS Medicinal Chemistry Letters in 2015.<a href=\"https:\/\/www.ambeed.com\/products\/18213-75-7.html\">Product Details of 18213-75-7<\/a> This article mentions the following:<\/p>\n<p>The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ss-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin. In order to explore the consequences of tankyrase and Wnt pathway inhibition in preclin. models of cancer and its impact on normal tissue, the authors sought a small mol. inhibitor of TNKS1\/2 with suitable physicochem. properties and pharmacokinetics for hypothesis testing in vivo. Starting from a 2-Ph quinazolinone hit <strong>I<\/strong>, the authors discovered the pyrrolopyrimidinone compound <strong>II<\/strong> (AZ6102), which is a potent TNKS1\/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. Moreover, compound <strong>II<\/strong> can be formulated well in a clin. relevant i.v. solution at 20 mg\/mL, has demonstrated good pharmacokinetics in preclin. species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7<a href=\"https:\/\/www.ambeed.com\/products\/18213-75-7.html\">Product Details of 18213-75-7<\/a>).<\/p>\n<p>5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.<a href=\"https:\/\/www.ambeed.com\/products\/18213-75-7.html\">Product Details of 18213-75-7<\/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>5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.<a href=\"https:\/\/www.ambeed.com\/products\/18213-75-7.html\">Product Details of 18213-75-7<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[538,131],"tags":[128],"class_list":["post-12168","post","type-post","status-publish","format-standard","hentry","category-18213-75-7","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. Ann;Casella, Robert;Croft, Rosemary A.;Dishington, Allan P.;Gingipalli, Lakshmaiah;Gu, Chungang;Hawkins, Janet L.;Holmes, Jane L.;Howard, Tina;Huang, Jian;Ioannidis, Stephanos;Kazmirski, Steven;Lamb, Michelle L.;McGuire, Thomas M.;Moore, Jane E.;Ogg, Derek;Patel, Anil;Pike, Kurt G.;Pontz, Timothy;Robb, Graeme R.;Su, Nancy;Wang, Haiyun;Wu, Xiaoyun;Zhang, Hai-Jun;Zhang, Yue;Zheng, Xiaolan;Wang, Tao. And the article was included in ACS Medicinal Chemistry Letters in 2015.Product Details of 18213-75-7 This article mentions the following:\" \/>\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=12168\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. Ann;Casella, Robert;Croft, Rosemary A.;Dishington, Allan P.;Gingipalli, Lakshmaiah;Gu, Chungang;Hawkins, Janet L.;Holmes, Jane L.;Howard, Tina;Huang, Jian;Ioannidis, Stephanos;Kazmirski, Steven;Lamb, Michelle L.;McGuire, Thomas M.;Moore, Jane E.;Ogg, Derek;Patel, Anil;Pike, Kurt G.;Pontz, Timothy;Robb, Graeme R.;Su, Nancy;Wang, Haiyun;Wu, Xiaoyun;Zhang, Hai-Jun;Zhang, Yue;Zheng, Xiaolan;Wang, Tao. And the article was included in ACS Medicinal Chemistry Letters in 2015.Product Details of 18213-75-7 This article mentions the following:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=12168\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2023-02-06T18:27:13+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=12168\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=12168\",\"name\":\"Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2023-02-06T18:27:13+00:00\",\"author\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. 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And the article was included in ACS Medicinal Chemistry Letters in 2015.Product Details of 18213-75-7 This article mentions the following:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=12168#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=12168\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=12168#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"http:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7\"}]},{\"@type\":\"WebSite\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"http:\/\/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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And the article was included in ACS Medicinal Chemistry Letters in 2015.Product Details of 18213-75-7 This article mentions the following:","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=12168","og_locale":"en_US","og_type":"article","og_title":"Johannes, Jeffrey W. et al. published their research in ACS Medicinal Chemistry Letters in 2015 | CAS: 18213-75-7 | pyrazoles-derivatives","og_description":"Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology was written by Johannes, Jeffrey W.;Almeida, Lynsie;Barlaam, Bernard;Boriack-Sjodin, P. 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