Discovery of 2-amino-6-carboxamidobenzothiazoles as potent Lck inhibitors

A novel series of 2-amino-6-carboxamidobenzothiazole was discovered to have potent Lck inhibitory properties. A highly efficient chemistry was developed. Also described are the detailed SAR study and the BaF3 cell line profiling for this series.

A novel series of 2-amino-6-carboxamidobenzothiazole was discovered to have potent Lck inhibitory properties. A highly efficient chemistry was developed. Many potent analogues were generated with urea, carbamate, heteroarylamine or alkylamine at the C-2 position. The SAR for the middle ring and the right side aryl group was also explored. The selectivity profile was herein included.Figure optionsDownload as PowerPoint slide