{"id":10077,"date":"2022-10-14T07:43:40","date_gmt":"2022-10-13T23:43:40","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10077"},"modified":"2022-10-14T07:43:40","modified_gmt":"2022-10-13T23:43:40","slug":"phillipson-louisa-j-s-team-published-research-in-bioorganic-medicinal-chemistry-in-2015-cas-844501-71-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10077","title":{"rendered":"Phillipson, Louisa J.&#8217;s team published research in Bioorganic &#038; Medicinal Chemistry in 2015 | CAS: 844501-71-9"},"content":{"rendered":"<p><a href=\"https:\/\/www.ambeed.com\/products\/844501-71-9.html\">Product Details of 844501-71-9<\/a>In 2015 ,\u300aDiscovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9\u300b appeared in Bioorganic &#038; Medicinal Chemistry. The author of the article were Phillipson, Louisa J.; Segal, David H.; Nero, Tracy L.; Parker, Michael W.; Wan, Soo San; de Silva, Melanie; Guthridge, Mark A.; Wei, Andrew H.; Burns, Christopher J.. The article conveys some information:<\/p>\n<p>The serine-threonine kinase CDK9 is a target of emerging interest for the development of anti-cancer drugs. There are multiple lines of evidence linking CDK9 activity to cancer, including the essential role this kinase plays in transcriptional regulation through phosphorylation of the C-terminal domain (CTD) of RNA polymerase II. Indeed, inhibition of CDK9 has been shown to result in a reduction of short-lived proteins such as the pro-survival protein Mcl-1 in malignant cells leading to the induction of apoptosis. In this work we report our initial studies towards the discovery of selective CDK9 inhibitors, starting from the known multi-kinase inhibitor PIK-75 which possesses potent CDK9 activity. Our series is based on a pyrazolo[1,5-a]pyrimidine nucleus and, importantly, the resultant lead compound 18b is devoid of the structural liabilities present in PIK-75 and possesses greater selectivity. The results came from multiple reactions, including the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9<a href=\"https:\/\/www.ambeed.com\/products\/844501-71-9.html\">Product Details of 844501-71-9<\/a>)<\/p>\n<p>3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/844501-71-9.html\">Product Details of 844501-71-9<\/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>3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/844501-71-9.html\">Product Details of 844501-71-9<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[745,131],"tags":[128],"class_list":["post-10077","post","type-post","status-publish","format-standard","hentry","category-844501-71-9","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>Phillipson, Louisa J.&#039;s team published research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 844501-71-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Product Details of 844501-71-9In 2015 ,\u300aDiscovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9\u300b appeared in Bioorganic &amp; Medicinal Chemistry. The author of the article were Phillipson, Louisa J.; Segal, David H.; Nero, Tracy L.; Parker, Michael W.; Wan, Soo San; de Silva, Melanie; Guthridge, Mark A.; Wei, Andrew H.; Burns, Christopher J.. The article conveys some information:\" \/>\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=10077\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Phillipson, Louisa J.&#039;s team published research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 844501-71-9 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Product Details of 844501-71-9In 2015 ,\u300aDiscovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9\u300b appeared in Bioorganic &amp; Medicinal Chemistry. The author of the article were Phillipson, Louisa J.; Segal, David H.; Nero, Tracy L.; Parker, Michael W.; Wan, Soo San; de Silva, Melanie; Guthridge, Mark A.; Wei, Andrew H.; Burns, Christopher J.. 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