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.
Huang
Shenlin
S
The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA. shuang2@gnf.org
Liu
Zuosheng
Z
Tian
Shin-Shay
SS
Sandberg
Mark
M
Spalding
Tracy A
TA
Romeo
Russell
R
Iskandar
Maya
M
Wang
Zhiliang
Z
Karanewsky
Donald
D
He
Yun
Y
D000818:Animals; D001402:B-Lymphocytes / Q000166:cytology / Q000187:drug effects*; D001549:Benzamides / Q000138:chemical synthesis / Q000494:pharmacology*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects*; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D051379:Mice; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D001549:Benzamides; D052160:Benzothiazoles; D047428:Protein Kinase Inhibitors; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)