Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.
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.
Kim
Kyung-Hee
KH
Wyeth Research, Chemical Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. kimk@wyeth.com
Wissner
Allan
A
Floyd
Middleton B
MB
Fraser
Heidi L
HL
Wang
Yanong D
YD
Dushin
Russell G
RG
Hu
Yongbo
Y
Olland
Andrea
A
Guo
Bing
B
Arndt
Kim
K
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
D000970:Antineoplastic Agents; D009287:Naphthyridines; D047428:Protein Kinase Inhibitors; D064413:3-Phosphoinositide-Dependent Protein Kinases; D017346:Protein Serine-Threonine Kinases