title: Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.
abstract: A series of substituted benzo[c][2,7]-naphthyridines were prepared and showed good potency in inhibiting PDK-1. The synthesis and SAR of this series of compounds are presented as well as the X-ray crystal structure of one of these analogs in a complex with PDK-1.
authors.affiliation: Wyeth Research, Chemical Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. kimk@wyeth.com
authors.forename: Kyung-Hee
authors.initials: KH
authors.lastname: Kim
authors.forename: Allan
authors.initials: A
authors.lastname: Wissner
authors.forename: Middleton B
authors.initials: MB
authors.lastname: Floyd
authors.forename: Heidi L
authors.initials: HL
authors.lastname: Fraser
authors.forename: Yanong D
authors.initials: YD
authors.lastname: Wang
authors.forename: Russell G
authors.initials: RG
authors.lastname: Dushin
authors.forename: Yongbo
authors.initials: Y
authors.lastname: Hu
authors.forename: Andrea
authors.initials: A
authors.lastname: Olland
authors.forename: Bing
authors.initials: B
authors.lastname: Guo
authors.forename: Kim
authors.initials: K
authors.lastname: Arndt
mesh_terms: D064413:3-Phosphoinositide-Dependent Protein Kinases; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D018360:Crystallography, X-Ray; D006801:Humans; D008968:Molecular Conformation; D009287:Naphthyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009287:Naphthyridines; D047428:Protein Kinase Inhibitors; D064413:3-Phosphoinositide-Dependent Protein Kinases; D017346:Protein Serine-Threonine Kinases