Abstract
A novel series of carbamates was discovered as potent and selective HER-2 sheddase inhibitors. Significant enhancement in potency and selectivity was achieved through attenuating the P1 moiety, which was conventionally believed to be exposed to solvent.
MeSH terms
-
Carbamates / chemical synthesis
-
Carbamates / chemistry*
-
Carbamates / pharmacology
-
Collagenases / metabolism
-
Humans
-
Microsomes, Liver / metabolism
-
Protein Kinase Inhibitors / chemical synthesis
-
Protein Kinase Inhibitors / chemistry*
-
Protein Kinase Inhibitors / pharmacology
-
Receptor, ErbB-2 / antagonists & inhibitors*
-
Receptor, ErbB-2 / metabolism
-
Structure-Activity Relationship
Substances
-
Carbamates
-
Protein Kinase Inhibitors
-
Receptor, ErbB-2
-
Collagenases