302963-99-1Relevant articles and documents
Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays
Parodi, Alice,Righetti, Giada,Pesce, Emanuela,Salis, Annalisa,Tasso, Bruno,Urbinati, Chiara,Tomati, Valeria,Damonte, Gianluca,Rusnati, Marco,Pedemonte, Nicoletta,Cichero, Elena,Millo, Enrico
, (2020/10/02)
Cystic fibrosis (CF) is the autosomal recessive disorder most recurrent in Caucasian populations. It is caused by different mutations in the cystic fibrosis transmembrane regulator protein (CFTR) gene, with F508del being the most common. During the last y
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck
Wityak, John,Das, Jagabandhu,Moquin, Robert V.,Shen, Zhongqi,Lin, James,Chen, Ping,Doweyko, Arthur M.,Pitt, Sidney,Pang, Suhong,Shen, Ding Ren,Fang, Qiong,De Fex, Henry F.,Schieven, Gary L.,Kanner, Steven B.,Barrish, Joel C.
, p. 4007 - 4010 (2007/10/03)
A novel series of 2-amino-5-carboxamidothiazoles were identified as inhibitors of Lck. Structure-activity studies demonstrate the structural requirements for potent Lck activity. Cyclopropylamide 11d is a potent Lck inhibitor having sub-micromolar activity in a PBL proliferation assay.