4862-94-6Relevant articles and documents
TGF-beta receptor inhibitor
-
Paragraph 0159-0160; 0162, (2021/04/28)
The invention provides a compound shown as a formula (I) and a pharmaceutical composition thereof. The compound shown as the formula (I) of the present invention is useful as a TGF-beta receptor inhibitor, particularly a TGF beta RI inhibitor, for example, in the prevention or treatment of various TGF beta RI (ALK5) mediated related diseases.
Design, synthesis and biological evaluation of GPR55 agonists
Fakhouri, Lara,Cook, Christopher D.,Al-Huniti, Mohammed H.,Console-Bram, Linda M.,Hurst, Dow P.,Spano, Michael B.S.,Nasrallah, Daniel J.,Caron, Marc G.,Barak, Larry S.,Reggio, Patricia H.,Abood, Mary E.,Croatt, Mitchell P.
, p. 4355 - 4367 (2017/07/22)
GPR55, a G protein-coupled receptor, is an attractive target to alleviate inflammatory and neuropathic pain and treat osteoporosis and cancer. Identifying a potent and selective ligand will aid to further establish the specific physiological roles and pharmacology of the receptor. Towards this goal, a targeted library of 22 compounds was synthesized in a modular fashion to obtain structure-activity relationship information. The general route consisted of coupling a variety of p-aminophenyl sulfonamides to isothiocyanates to form acylthioureas. For the synthesis of a known naphthyl ethyl alcohol motif, route modification led to a shorter and more efficient process. The 22 analogues were analyzed for their ability to serve as agonists at GPR55 and valuable information for both ends of the molecule was ascertained.
Synthesis and biological activity of N-aryl-2-aminothiazoles: Potent pan inhibitors of cyclin-dependent kinases
Misra, Raj N.,Xiao, Hai-Yun,Williams, David K.,Kim, Kyoung S.,Lu, Songfeng,Keller, Kristen A.,Mulheron, Janet G.,Batorsky, Roberta,Tokarski, John S.,Sack, John S.,Kimball, S. David,Lee, Francis Y.,Webster, Kevin R.
, p. 2973 - 2977 (2007/10/03)
N-Aryl aminothiazoles 6-9 were prepared from 2-bromothiazole 5 and found to be CDK inhibitors. In cells they act as potent cytotoxic agents. Selectivity for CDK1, CDK2, and CDK4 was dependent of the nature of the N-aryl group and distinct from the CDK2 se