Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 7, 2010, Pages 2283-2286

  Lockman, Jeffrey W ^a   Reeder, Matthew D ^a   Suzuki, Kazuyuki ^a   Ostanin, Kirill ^a   Hoff, Ryan ^a   Bhoite, Leena ^a   Austin, Harry ^a   Baichwal, Vijay ^a   Adam Willardsen, J ^a  

^a Myriad Pharmaceuticals   (United States)

Author keywords

eEF2 K; Kinase; Thieno 2,3 b pyridine

Indexed keywords

4 AMINOPYRIMIDINE; AMIDE; ELONGATION FACTOR 2 KINASE; HETEROCYCLIC COMPOUND; LEAD; NITROGEN; PYRIMIDINE DERIVATIVE; THIENO[2,3 B]PYRIDINE DERIVATIVE; THIENOPYRIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CYTOTOXICITY; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MOLECULE; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

CELL LINE, TUMOR; CELL SURVIVAL; ELONGATION FACTOR 2 KINASE; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EUKARYOTA;

EID: 77949490412     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.005     Document Type: Article

References (21)

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18. 1H NMR.
19. Compound 16 is typical: Cyclooctanone (1 equiv), 3-methylbutanal (1 equiv), and KOH (2 equiv) are stirred in MeOH at rt for 3 h. 2-Cyanothioacetamide (1 equiv) and NaOMe (3 equiv) are added and the solution heated at reflux overnight. 2-Bromoacetamide (1 equiv) and NaOMe (1 equiv) are added and the reaction mixture heated at reflux until product is observed by LC/MS. The solution is concentrated and purified by RP-HPLC.
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