title: Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.
abstract: Several series of thieno[2-3-b]pyridine analogues were synthesized and screened for inhibitory activity against eukaryotic elongation factor-2 kinase (eEF2-K). Modifications around several regions of the lead molecules were made, with a ring fusion adjacent to the nitrogen on the thienopyridine core being critical for activity. The most active compound 34 shows an IC(50) of 170 nM against eEF2-K in vitro.
authors.affiliation: Department of Medicinal Chemistry, Myriad Pharmaceuticals, 305 Chipeta Way, Salt Lake City, UT 84108, United States. jeffrey.lockman@myriadpharma.com
authors.forename: Jeffrey W
authors.initials: JW
authors.lastname: Lockman
authors.forename: Matthew D
authors.initials: MD
authors.lastname: Reeder
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Suzuki
authors.forename: Kirill
authors.initials: K
authors.lastname: Ostanin
authors.forename: Ryan
authors.initials: R
authors.lastname: Hoff
authors.forename: Leena
authors.initials: L
authors.lastname: Bhoite
authors.forename: Harry
authors.initials: H
authors.lastname: Austin
authors.forename: Vijay
authors.initials: V
authors.lastname: Baichwal
authors.forename: J
authors.initials: J
authors.lastname: Adam Willardsen
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D054736:Elongation Factor 2 Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; C446540:thienopyridine; D054736:Elongation Factor 2 Kinase