Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.
A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC(50) of less than 1 nM against wild-type Bcr-Abl and an EC(50) of 10 nM against T315I mutant but is broadly active against a number of other kinases.
Deng
Xianming
X
Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, United States.
Lim
Sang Min
SM
Zhang
Jianming
J
Gray
Nathanael S
NS
D000480:Alkynes / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000480:Alkynes; D001549:Benzamides; C000605795:HG-6-63-01; D011725:Pyridines; D016044:Fusion Proteins, bcr-abl