Discovery and in vitro evaluation of potent kinase inhibitors:: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines

被引:31
|
作者
Alberti, MJ [1 ]
Auten, EP [1 ]
Lackey, KE [1 ]
McDonald, OB [1 ]
Wood, ER [1 ]
Preugschat, F [1 ]
Cutler, GJ [1 ]
Kane-Carson, L [1 ]
Liu, W [1 ]
Jung, DK [1 ]
机构
[1] GlaxoSmithKline Inc, Res Triangle Pk, NC 27709 USA
关键词
kinase inhibitor; VEGFR; GSK; Erb; EGFR;
D O I
10.1016/j.bmcl.2005.05.100
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 several pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines as potent kinase inhibitors are discussed. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3778 / 3781
页数:4
相关论文
共 50 条
  • [31] SYNTHESIS OF NEW PYRIDO[2′,3′:3,4] PYRAZOLO[1,5-a] PYRIMIDINES AND THEIR USE IN THE PREPARATION OF TETRAHETEROCYCLIC SYSTEMS
    El-Essawy, Farag A.
    SYNTHETIC COMMUNICATIONS, 2010, 40 (06) : 877 - 887
  • [32] PREPARATION OF SOME 1- AND 2-BETA-D-RIBOFURANOSYL-PYRAZOLO[3,4-D]PYRIMIDINES
    DAVOLL, J
    KERIDGE, KA
    JOURNAL OF THE CHEMICAL SOCIETY, 1961, (JUN): : 2589 - &
  • [33] Regioselectivity of 1,3-dipolar cycloadditions and antimicrobial activity of isoxazoline, pyrrolo[3,4-d]isoxazole-4,6-diones, pyrazolo[3,4-d]pyridazines and pyrazolo[1,5-a]pyrimidines
    Zaki, Yasser Hassan
    Sayed, Abdelwahed Rashad
    Elroby, Shaaban A.
    CHEMISTRY CENTRAL JOURNAL, 2016, 10
  • [34] Regioselectivity of 1,3-dipolar cycloadditions and antimicrobial activity of isoxazoline, pyrrolo[3,4-d]isoxazole-4,6-diones, pyrazolo[3,4-d]pyridazines and pyrazolo[1,5-a]pyrimidines
    Yasser Hassan Zaki
    Abdelwahed Rashad Sayed
    Shaaban A. Elroby
    Chemistry Central Journal, 10
  • [35] REACTIONS OF URACILS .3. PYRAZOLO[3,4-D]PYRIMIDINES AND PYRIDO[2,3-D]PYRIMIDINES FROM 5-FORMYL-1,3-DIMETHYLURACILS
    MATYUS, P
    SOHAR, P
    WAMHOFF, H
    HETEROCYCLES, 1984, 22 (03) : 513 - 518
  • [36] Synthesis and biological evaluation of a series of substituted pyrazolo [3,4-d]-1,2,3-triazoles and pyrazolo[3,4-d]oxazoles
    Vicentini, CB
    Manfredini, S
    Manfrini, M
    Bazzanini, R
    Musiu, C
    Putzolu, M
    Perra, G
    Marongiu, ME
    ARCHIV DER PHARMAZIE, 1998, 331 (09) : 269 - 272
  • [37] In silico screening of a series of 1,6-disubstituted 1H-pyrazolo[3,4-d]pyrimidines as potential selective inhibitors of the Janus kinase 3
    Faris, Abdelmoujoud
    Hadni, Hanine
    Saleh, Basil A.
    Khelfaoui, Hadjer
    Harkati, Dalal
    Ait Ahsaine, Hassan
    Elhallaoui, Menana
    El-Hiti, Gamal A.
    JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2023, : 4456 - 4474
  • [38] Synthesis, anticancer evaluation, molecular docking and ADME study of novel pyrido[4ʹ,3ʹ:3,4]pyrazolo[1,5-a]pyrimidines as potential tropomyosin receptor kinase A (TrKA) inhibitors
    Nadia Hanafy Metwally
    Emad Abdullah Deeb
    Ibrahim Walid Hasani
    BMC Chemistry, 18
  • [39] Synthesis, anticancer evaluation, molecular docking and ADME study of novel pyrido[4′,3′:3,4]pyrazolo[1,5-a]pyrimidines as potential tropomyosin receptor kinase A (TrKA) inhibitors
    Metwally, Nadia Hanafy
    Deeb, Emad Abdullah
    Hasani, Ibrahim Walid
    BMC CHEMISTRY, 2024, 18 (01)
  • [40] Design, synthesis and brief SAR of pyrazolo[3,4-d] and pyrrolo[2,3-d]pyrimidines as potent inhibitors of LCK.
    Burchat, AF
    Calderwood, DJ
    Deng, BJ
    Friedman, M
    Hirst, G
    Li, BQ
    Ritter, K
    Skinner, B
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U25 - U25