title: Fused thiophene derivatives as MEK inhibitors.
abstract: A number of novel fused thiophene derivatives have been prepared and identified as potent inhibitors of MEK. The SAR data of selected examples and the in vivo profiling of compound 13 h demonstrates the functional activity of this class of compounds in HT-29 PK/PD models.
authors: Department of Medicinal Chemistry, UCB Pharma, 216 Bath Road, Slough, Berkshire SL1 3WE, UK. victoria.jackson@ucb.com
authors: Victoria E
authors: VE
authors: Laing
authors: Daniel C
authors: DC
authors: Brookings
authors: Rachel J
authors: RJ
authors: Carbery
authors: Jose Gascon
authors: JG
authors: Simorte
authors: Martin C
authors: MC
authors: Hutchings
authors: Barry J
authors: BJ
authors: Langham
authors: Martin A
authors: MA
authors: Lowe
authors: Rodger A
authors: RA
authors: Allen
authors: Joanne R
authors: JR
authors: Fetterman
authors: James
authors: J
authors: Turner
authors: Christoph
authors: C
authors: Meier
authors: Jeff
authors: J
authors: Kennedy
authors: Mark
authors: M
authors: Merriman
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D020930:MAP Kinase Kinase Kinases / Q000037:antagonists & inhibitors*; D051379:Mice; D008956:Models, Chemical; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D055672:Static Electricity; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry*; D013997:Time Factors
chemical_list: D047428:Protein Kinase Inhibitors; D013876:Thiophenes; D020930:MAP Kinase Kinase Kinases