title: Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.
abstract: The thieno[2,3-b]pyridine-5-carbonitrile with a 5-indolylamine at C-4 and a phenyl group at C-2 had a moderate activity against PKCtheta. Optimization of the groups at C-4 and C-2 led to analog 29, which has an IC(50) value of 7.5nM for the inhibition of PKCtheta.
authors.affiliation: Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. bosched@wyeth.com
authors.forename: Diane H
authors.initials: DH
authors.lastname: Boschelli
authors.forename: Biqi
authors.initials: B
authors.lastname: Wu
authors.forename: Ana Carolina
authors.initials: AC
authors.lastname: Barrios Sosa
authors.forename: Joan
authors.initials: J
authors.lastname: Chen
authors.forename: Magda
authors.initials: M
authors.lastname: Asselin
authors.forename: Derek C
authors.initials: DC
authors.lastname: Cole
authors.forename: Julie
authors.initials: J
authors.lastname: Lee
authors.forename: Xiaoke
authors.initials: X
authors.lastname: Yang
authors.forename: Divya
authors.initials: D
authors.lastname: Chaudhary
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects / Q000473:pathology; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D051379:Mice; D018345:Mice, Knockout; D008956:Models, Chemical; D009570:Nitriles / Q000138:chemical synthesis / Q000494:pharmacology*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007527:Isoenzymes; D009570:Nitriles; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D013876:Thiophenes; D011493:Protein Kinase C