Sawyer, J. Scott; Beight, Douglas W.; Britt, Karen S.; Anderson, Bryan D.; Campbell, Robert M.; Goodson, Theodore; Herron, David K.; Li, Hong-Yu; McMillen, William T.; Mort, Nicholas; Parsons, Stephen; Smith, Edward C. R.; Wagner, Jill R.; Yan, Lei; Zhang, Faming; Yingling, Jonathan M. published the artcile< Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain>, SDS of cas: 658-99-1, the main research area is dihydropyrrolopyrazole preparation transforming growth factor receptor kinase domain inhibitor; pyrrolopyrazole dihydro aryl heteroaryl preparation; pyrazole heteroaryl preparation structure activity relationship growth factor inhibitor; crystal structure dihydropyrrolopyrazole phenyl quinolinyl bound kinase domain.
We have expanded our previously reported series of pyrazole-based inhibitors of the TGF-β type I receptor kinase domain (TβR-I) to now include new 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole analogs. Limited examination of the SAR of this new series in both enzyme and cell based in vitro assays has revealed selectivity differences with respect to p38 MAP kinase (p38 MAPK) depending on the nature of the warhead’ group on the dihydropyrrolopyrazole ring. As with our original pyrazole series, Ph substituents tended to show greater selectivity against p38 MAPK than those comprised of the quinoline-4-yl moiety. We have also achieved co-crystallization and X-ray anal. of compounds I and II, two potent examples of this new series, with the TβR-I receptor kinase domain.
Bioorganic & Medicinal Chemistry Letters published new progress about Animal cell line (p3TP Lux). 658-99-1 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H5F2N, SDS of cas: 658-99-1.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts