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Bioorg Med Chem Lett ; 22(1): 472-5, 2012 Jan 01.
Article in English | MEDLINE | ID: mdl-22119475

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.


Subject(s)
Chemistry, Pharmaceutical/methods , MAP Kinase Kinase Kinases/antagonists & inhibitors , Protein Kinase Inhibitors/pharmacology , Thiophenes/chemistry , Animals , Cell Line, Tumor , Crystallography, X-Ray/methods , Drug Design , Drug Screening Assays, Antitumor , Humans , Inhibitory Concentration 50 , Mice , Models, Chemical , Phosphorylation , Static Electricity , Structure-Activity Relationship , Time Factors
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