Novel protein kinase C inhibitors:: Synthesis and PKC inhibition of β-substituted polythiophene derivatives

被引:26
|
作者
Xu, WC
Zhou, Q
Ashendel, CL
Chang, CT
Chang, CJ [1 ]
机构
[1] Purdue Univ, Sch Pharm, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA
[2] Union Chem Labs, Hsinchu, Taiwan
关键词
D O I
10.1016/S0960-894X(99)00375-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of beta-substituted polythiophene derivatives was synthesized through palladium-catalyzed coupling reaction. Their structure-protein kinase C (PKC) inhibitory activity relationship was studied. The carboxaldehyde and hydroxymethyl derivatives of alpha-terthiophene were potent PKC inhibitors (IC50 = 10(-7) M). (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2279 / 2282
页数:4
相关论文
共 50 条
  • [1] Synthesis and biological evaluation of novel protein kinase C (PKC) inhibitors.
    Sham, KKC
    Daines, RA
    Kingsbury, WD
    Hofmann, GA
    Mattern, MR
    Nambi, P
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 213 : 202 - MEDI
  • [2] Novel protein kinase C inhibitors:: α-terthiophene derivatives
    Kim, DSHL
    Ashendel, CL
    Zhou, Q
    Chang, CT
    Lee, ES
    Chang, CJ
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (19) : 2695 - 2698
  • [3] Bradykinin potentiation by ACE inhibitors: Inhibition of metabolism, protein kinase C (PKC) or phosphatases?
    Tom, B
    de Vries, R
    Saxena, PR
    Danser, AH
    HYPERTENSION, 2001, 38 (03) : 499 - 499
  • [4] THE SYNTHESIS AND ACTIVITY OF SUBSTITUTED (AMINOMETHYL)PIPERIDINES - A NOVEL CLASS OF SELECTIVE PROTEIN-KINASE-C INHIBITORS
    SHEARER, BG
    SULLIVAN, JP
    CARTER, JP
    MATHEW, RM
    WAID, P
    CONNOR, JR
    PATCH, CKRJ
    BURCH, RM
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1991, 202 : 25 - MEDI
  • [5] Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα (PKCα) activators
    Hirai, Go
    Ogoshi, Yosuke
    Ohkubo, Megumi
    Tamura, Yuki
    Watanabe, Toru
    Shimizu, Tadashi
    Sodeoka, Mikiko
    TETRAHEDRON LETTERS, 2009, 50 (26) : 3609 - 3612
  • [6] NOVEL SUBSTITUTED INDOLOCARBAZOLES AS POTENT AND SELECTIVE INHIBITORS OF PROTEIN-KINASE-C
    XIE, GJ
    NAGATA, H
    TAMAOKI, T
    LOWN, JW
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (23) : 2841 - 2844
  • [7] Inhibition of the activity of protein kinase C (PKC) isoforms by bioflavonoids
    Joseph, CK
    Kabayama, M
    Ali, M
    Lok, HM
    Clark, H
    FASEB JOURNAL, 2003, 17 (05): : A1339 - A1339
  • [8] SYNTHESIS OF NOVEL OXINDOLE DERIVATIVES AS INHIBITORS OF C-SRC TYROSINE KINASE
    Kurt, Z. K.
    Olgen, S.
    EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2011, 44 : 189 - 190
  • [9] Selective protein kinase Cθ (PKCθ) inhibitors for the treatment of autoimmune diseases
    Curnock, Adam
    Bolton, Clare
    Chiu, Peter
    Doyle, Elisabeth
    Fraysse, Damien
    Hesse, Matthias
    Jones, Julie
    Weber, Peter
    Jimenez, Juan-Miguel
    BIOCHEMICAL SOCIETY TRANSACTIONS, 2014, 42 : 1524 - 1528
  • [10] High throughput screen for inhibitors of protein kinase C iota (PKCι)
    Bisset, Louise
    Hammonds, Tim
    Roffey, Jon
    Kelland, Lloyd
    Travers, Jon
    Parker, Peter
    Kjaer, Svend
    McDonald, Neil
    MOLECULAR CANCER THERAPEUTICS, 2007, 6 (12) : 3512S - 3512S