{"id":9995,"date":"2022-10-13T03:03:03","date_gmt":"2022-10-12T19:03:03","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9995"},"modified":"2022-10-13T03:03:03","modified_gmt":"2022-10-12T19:03:03","slug":"le-brazidec-jean-yvess-team-published-research-in-bioorganic-medicinal-chemistry-letters-in-2012-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9995","title":{"rendered":"Le Brazidec, Jean-Yves’s team published research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 847818-74-0"},"content":{"rendered":"

Product Details of 847818-74-0<\/a>In 2012 ,\u300aStructure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors\u300b appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Le Brazidec, Jean-Yves; Pasis, Angela; Tam, Betty; Boykin, Christina; Wang, Deping; Marcotte, Douglas J.; Claassen, Gisela; Chong, Jer-Hong; Chao, Jianhua; Fan, Junhua; Nguyen, Khanh; Silvian, Laura; Ling, Leona; Zhang, Lin; Choi, Michael; Teng, Min; Pathan, Nuzhat; Zhao, Shuo; Li, Tony; Taveras, Art. The article conveys some information:<\/p>\n

This Letter reports the optimization of a pyrrolopyrimidine series as dual inhibitors of Aurora A\/B kinases. This series is derived from a pyrazolopyrimidine series previously reported as inhibitors of aurora kinases and CDKs. In an effort to improve the selectivity of this chemotype, we switched to the pyrrolopyrimidine core which allowed functionalization on C-2. In addition, the modeling rationale was based on superimposing the structures of Aurora-A kinase and CDK2 which revealed enough differences leading to a path for selectivity improvement. The synthesis of the new series of pyrrolopyrimidine analogs relied on the development of a different route for the two key intermediates, which led to analogs with both tunable activity against CDK1 and maintained cell potency. The experimental process involved the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Product Details of 847818-74-0<\/a>)<\/p>\n

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. Product Details of 847818-74-0<\/a><\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

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. Product Details of 847818-74-0<\/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-9995","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nLe Brazidec, Jean-Yves's team published research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Product Details of 847818-74-0In 2012 ,\u300aStructure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors\u300b appeared in Bioorganic & Medicinal Chemistry Letters. 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