Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles

被引:114
作者
Wood, ER [1 ]
Kuyper, L [1 ]
Petrov, KG [1 ]
Hunter, RN [1 ]
Harris, PA [1 ]
Lackey, K [1 ]
机构
[1] GlaxoSmithKline, Res Triangle Pk, NC 27709 USA
关键词
TrkA kinase inhibitors;
D O I
10.1016/j.bmcl.2003.12.002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The discovery, synthesis, potential binding mode, and in vitro kinase profile of 3-(3-bromo-4-hydroxy-5-(2'-methoxyphenyl)-benzylidene)-5-bromo-1,3-dihydro-pyrrolo[2,3-b]-pyridin-2-one, 3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one as potent TrkA inhibitors are discussed. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:953 / 957
页数:5
相关论文
共 20 条
  • [1] Kinetics of trkA tyrosine kinase activity and inhibition by K-252a
    Angeles, TS
    Yang, SX
    Steffler, C
    Dionne, CA
    [J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1998, 349 (02) : 267 - 274
  • [2] Pancreatic cancer biology and genetics
    Bardeesy, N
    DePinho, RA
    [J]. NATURE REVIEWS CANCER, 2002, 2 (12) : 897 - 909
  • [3] Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): Design, synthesis, enzymatic activities, and X-ray crystallographic analysis
    Bramson, HN
    Corona, J
    Davis, ST
    Dickerson, SH
    Edelstein, M
    Frye, SV
    Gampe, RT
    Harris, PA
    Hassell, A
    Holmes, WD
    Hunter, RN
    Lackey, KE
    Lovejoy, B
    Luzzio, MJ
    Montana, V
    Rocque, WJ
    Rusnak, D
    Shewchuk, L
    Veal, JM
    Walker, DH
    Kuyper, LF
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (25) : 4339 - 4358
  • [4] Descamps S, 2001, CANCER RES, V61, P4337
  • [5] Dionne CA, 1998, CLIN CANCER RES, V4, P1887
  • [6] Frade JM, 1998, BIOESSAYS, V20, P137, DOI 10.1002/(SICI)1521-1878(199802)20:2<137::AID-BIES6>3.0.CO
  • [7] 2-Q
  • [8] Guate JL, 1999, BJU INT, V84, P495
  • [9] Signal transduction by the neurotrophin receptors
    Kaplan, DR
    Miller, FD
    [J]. CURRENT OPINION IN CELL BIOLOGY, 1997, 9 (02) : 213 - 221
  • [10] The discovery of potent cRaf1 kinase inhibitors
    Lackey, K
    Cory, M
    Davis, R
    Frye, SV
    Harris, PA
    Hunter, RN
    Jung, DK
    McDonald, OB
    McNutt, RW
    Peel, MR
    Rutkowske, RD
    Veal, JM
    Wood, ER
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (03) : 223 - 226