title: N3-arylmalonamides: a new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases.
abstract: A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC(50) values in the low nanomolar range in vitro and were efficacious in human tumor xenograft models in mice in vivo.
authors.affiliation: Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, QC, Canada H4S 2A1.
authors.forename: Oscar
authors.initials: O
authors.lastname: Saavedra
authors.forename: Stephen
authors.initials: S
authors.lastname: Claridge
authors.forename: Lijie
authors.initials: L
authors.lastname: Zhan
authors.forename: Franck
authors.initials: F
authors.lastname: Raeppel
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Granger
authors.forename: Stéphane
authors.initials: S
authors.lastname: Raeppel
authors.forename: Michael
authors.initials: M
authors.lastname: Mannion
authors.forename: Frédéric
authors.initials: F
authors.lastname: Gaudette
authors.forename: Nancy
authors.initials: N
authors.lastname: Zhou
authors.forename: Ljubomir
authors.initials: L
authors.lastname: Isakovic
authors.forename: Naomy
authors.initials: N
authors.lastname: Bernstein
authors.forename: Robert
authors.initials: R
authors.lastname: Déziel
authors.forename: Hannah
authors.initials: H
authors.lastname: Nguyen
authors.forename: Normand
authors.initials: N
authors.lastname: Beaulieu
authors.forename: Carole
authors.initials: C
authors.lastname: Beaulieu
authors.forename: Isabelle
authors.initials: I
authors.lastname: Dupont
authors.forename: James
authors.initials: J
authors.lastname: Wang
authors.forename: A Robert
authors.initials: AR
authors.lastname: Macleod
authors.forename: Jeffrey M
authors.initials: JM
authors.lastname: Besterman
authors.forename: Arkadii
authors.initials: A
authors.lastname: Vaisburg
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D006801:Humans; D008314:Malonates / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D008314:Malonates; D047428:Protein Kinase Inhibitors; D011725:Pyridines; C446540:thienopyridine; D019859:Proto-Oncogene Proteins c-met; D040301:Vascular Endothelial Growth Factor Receptor-2; C008314:malonamide