Synthesis of small molecule CDC25 phosphatases inhibitors

被引:25
作者
Contour-Galcéra, MO
Lavergne, O
Brezak, MC
Ducommun, B
Prévost, G
机构
[1] Inst Henri Beaufour, Ipsen Res Labs, F-91966 Les Ulis, France
[2] Univ Toulouse 3, CNRS UMR 5088, LBCMCP, IFR109,Inst Explorat Fonct Genomes, F-31062 Toulouse, France
关键词
CDC25; inhibitor; dual specificity phosphatases inhibitor; antiproliferative agent;
D O I
10.1016/j.bmcl.2004.09.041
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A targeted library of small molecules has been prepared to optimize the biological activity of BN82002, our initial lead compound, recently described as an original inhibitor of CDC25 phosphatases. Some of these compounds inhibit CDC25 in the micromolar range and therefore reinforce the interest of CDC25 as an anticancer target. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5809 / 5812
页数:4
相关论文
共 15 条
  • [2] AUVIN S, 2000, Patent No. 0017190
  • [3] Novel synthetic inhibitor of CDC25 phosphatases:: BN82002
    Brezak, MC
    Quaranta, M
    Mondésert, O
    Galcera, MO
    Lavergne, O
    Alby, F
    Cazales, M
    Baldin, W
    Thurieau, C
    Harnett, J
    Lanco, C
    Kasprzyk, PG
    Prevost, GP
    Ducommun, B
    [J]. CANCER RESEARCH, 2004, 64 (09) : 3320 - 3325
  • [4] Cdc25 as a potential target of anticancer agents
    Eckstein, JW
    [J]. INVESTIGATIONAL NEW DRUGS, 2000, 18 (02) : 149 - 156
  • [5] Gasparotto D, 1997, CANCER RES, V57, P2366
  • [6] CDC25 IS A SPECIFIC TYROSINE PHOSPHATASE THAT DIRECTLY ACTIVATES P34CDC2
    GAUTIER, J
    SOLOMON, MJ
    BOOHER, RN
    BAZAN, JF
    KIRSCHNER, MW
    [J]. CELL, 1991, 67 (01) : 197 - 211
  • [7] Expression and functional significance of CDC25B in human pancreatic ductal adenocarcinoma
    Guo, JC
    Kleeff, J
    Li, JS
    Ding, JY
    Hammer, J
    Zhao, YP
    Giese, T
    Korc, M
    Büchler, MW
    Friess, H
    [J]. ONCOGENE, 2004, 23 (01) : 71 - 81
  • [8] Studies on menadione as an inhibitor of the cdc25 phosphatase
    Ham, SW
    Park, HJ
    Lim, DH
    [J]. BIOORGANIC CHEMISTRY, 1997, 25 (01) : 33 - 36
  • [9] Use of solid supported nucleophiles and electrophiles for the purification of non-peptide small molecule libraries
    Kaldor, SW
    Siegel, MG
    Fritz, JE
    Dressman, BA
    Hahn, PJ
    [J]. TETRAHEDRON LETTERS, 1996, 37 (40) : 7193 - 7196
  • [10] THE CDC25 PROTEIN CONTROLS TYROSINE DEPHOSPHORYLATION OF THE CDC2 PROTEIN IN A CELL-FREE SYSTEM
    KUMAGAI, A
    DUNPHY, WG
    [J]. CELL, 1991, 64 (05) : 903 - 914