Tag: 200-300

Product Details of 847818-74-0In 2012 ,《Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors》 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:

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)

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

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Application of 847818-74-0In 2015 ,《Discovery and Optimization of a Porcupine Inhibitor》 appeared in Journal of Medicinal Chemistry. The author of the article were Duraiswamy, Athisayamani Jeyaraj; Lee, May Ann; Madan, Babita; Ang, Shi Hua; Tan, Eldwin Sum Wai; Cheong, Wei Wen Vivien; Ke, Zhiyuan; Pendharkar, Vishal; Ding, Li Jun; Chew, Yun Shan; Manoharan, Vithya; Sangthongpitag, Kanda; Alam, Jenefer; Poulsen, Anders; Ho, Soo Yei; Virshup, David M.; Keller, Thomas H.. The article conveys some information:

Wnt proteins regulate various cellular functions and serve distinct roles in normal development throughout life. Wnt signaling is dysregulated in various diseases including cancers. Porcupine (PORCN) is a membrane-bound O-acyltransferase that palmitoleates the Wnts and hence is essential for their secretion and function. The inhibition of PORCN could serve as a therapeutic approach for the treatment of a number of Wnt-dependent cancers. Herein, the authors describe the identification of a Wnt secretion inhibitor from cellular high throughput screening. Classical SAR based cellular optimization provided us with a PORCN inhibitor I with nanomolar activity and excellent bioavailability that demonstrated efficacy in a Wnt-driven murine tumor model. Finally, the authors also discovered that enantiomeric PORCN inhibitors show very different activity in the reporter assay, suggesting that such compounds may be useful for mode of action studies on the PORCN O-acyltransferase. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 847818-74-0)

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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Application of 847818-74-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics