title: Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.
abstract: 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.
authors.affiliation: Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, United States.
authors.forename: Xianming
authors.initials: X
authors.lastname: Deng
authors.forename: Sang Min
authors.initials: SM
authors.lastname: Lim
authors.forename: Jianming
authors.initials: J
authors.lastname: Zhang
authors.forename: Nathanael S
authors.initials: NS
authors.lastname: Gray
mesh_terms: 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
chemical_list: D000480:Alkynes; D001549:Benzamides; C000605795:HG-6-63-01; D011725:Pyridines; D016044:Fusion Proteins, bcr-abl