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
  • [1] BRIDGEHEAD NITROGEN-HETEROCYCLES .7. THE SYNTHESIS OF SUBSTITUTED PYRIDO[1',2'-1,5]PYRAZOLO[3,4-D]PYRIMIDINES
    MOLINA, P
    ARQUES, A
    HERNANDEZ, H
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 1984, 21 (03) : 685 - 688
  • [2] Synthesis and in vitro anticancer activity of pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-d][1,2,3]triazines
    Hassan, Ashraf S.
    Moustafa, Gaber O.
    Awad, Hanem M.
    SYNTHETIC COMMUNICATIONS, 2017, 47 (21) : 1963 - 1972
  • [3] Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
    Greco, Chiara
    Catania, Rosa
    Balacco, Dario Leonardo
    Taresco, Vincenzo
    Musumeci, Francesca
    Alexander, Cameron
    Huett, Alan
    Schenone, Silvia
    MOLECULES, 2020, 25 (22):
  • [4] Synthesis of pyrrolino[3,4-d]pyrazoles, pyrazoles, pyrazolo[5,4-d]pyrimidines and pyrazolo[3,4-d]pyrimidines
    Riheem, Nadia A. Abdel
    Rateb, Nora M.
    Eldin, Sanaa M.
    DRUGS OF THE FUTURE, 2007, 32 : 40 - 41
  • [5] 1H-Pyrazolo[3,4-d]pyrimidines as potent and selective ATP-competitive mTOR inhibitors
    Kaplan, Joshua
    Curran, Kevin
    Richard, David
    Verheijen, Jeroen
    Yu, Ker
    Toral-Barza, Lourdes
    Zhang, Wei-Guo
    Lucas, Judy
    Hollander, Irwin
    Ayral-Kaloustian, Semiramis
    Mansour, Tarek
    Zask, Arie
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 238
  • [6] Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors
    Takarada, Jessica E.
    Cunha, Micael R.
    Almeida, Vitor M.
    Vasconcelos, Stanley N. S.
    Santiago, Andre S.
    Godoi, Paulo H.
    Salmazo, Anita
    Ramos, Priscila Z.
    Fala, Angela M.
    De Souza, Lucas R.
    Da Silva, Italo E. P.
    Bengtson, Mario H.
    Massirer, Katlin B.
    Counago, Rafael M.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2024, 98
  • [7] Pyrazolo[3,4-b]pyridine in heterocyclic synthesis:: synthesis of new pyrazolo[3,4-b]pyridines, imidazo[1′,2′:1,5]pyrazolo[3,4-b]pyridines, and pyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidines
    Gad-Elkareem, Mohamed A. M.
    Abdel-Fattah, Azza M.
    Elneairy, Mohamed A. A.
    CANADIAN JOURNAL OF CHEMISTRY, 2007, 85 (09) : 592 - 599
  • [8] Antifungal evaluation of substituted pyrazolo[3,4-d]pyrimidines
    Peixoto, F.
    Sivasubramanian, A.
    Abreu, C. G.
    Rodrigues, L. M.
    Oliveira-Campos, A. M. F.
    PROCEEDINGS OF THE SECOND IBERIAN CONGRESS ON CHESTNUT, 2008, (784): : 193 - 196
  • [9] Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors
    Xia, Y
    Chackalamannil, S
    Czarniecki, M
    Tsai, HG
    Vaccaro, H
    Cleven, R
    Cook, J
    Fawzi, A
    Watkins, R
    Zhang, HT
    JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (26) : 4372 - 4377
  • [10] STUDIES ON PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES .5. TRANSFORMATION OF PYRAZOLO[3,4-D]PYRIMIDINES-H-1 INTO PYRAZOLO[3,4-B]PYRIDINES-H-1
    HIGASHINO, T
    IWAI, Y
    HAYASHI, E
    CHEMICAL & PHARMACEUTICAL BULLETIN, 1977, 25 (04) : 535 - 542