Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties.
Wallace
Michael B
MB
Takeda San Diego, 10410 Science Center Drive, San Diego, CA 92121, United States. michael.wallace@takedasd.com
Adams
Mark E
ME
Kanouni
Toufike
T
Mol
Clifford D
CD
Dougan
Douglas R
DR
Feher
Victoria A
VA
O'Connell
Shawn M
SM
Shi
Lihong
L
Halkowycz
Petro
P
Dong
Qing
Q
D000818:Animals; D018360:Crystallography, X-Ray; D015195:Drug Design; D020930:MAP Kinase Kinase Kinases / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats
D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D020930:MAP Kinase Kinase Kinases