title: Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
abstract: 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.
authors.affiliation: Takeda San Diego, 10410 Science Center Drive, San Diego, CA 92121, United States. michael.wallace@takedasd.com
authors.forename: Michael B
authors.initials: MB
authors.lastname: Wallace
authors.forename: Mark E
authors.initials: ME
authors.lastname: Adams
authors.forename: Toufike
authors.initials: T
authors.lastname: Kanouni
authors.forename: Clifford D
authors.initials: CD
authors.lastname: Mol
authors.forename: Douglas R
authors.initials: DR
authors.lastname: Dougan
authors.forename: Victoria A
authors.initials: VA
authors.lastname: Feher
authors.forename: Shawn M
authors.initials: SM
authors.lastname: O'Connell
authors.forename: Lihong
authors.initials: L
authors.lastname: Shi
authors.forename: Petro
authors.initials: P
authors.lastname: Halkowycz
authors.forename: Qing
authors.initials: Q
authors.lastname: Dong
mesh_terms: 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
chemical_list: D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D020930:MAP Kinase Kinase Kinases