Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas

被引：37
作者：
Peng, Hao [2 ,3 ]
Liang, Yongju [1 ]
Chen, Le [2 ,3 ]
Fu, Liwu [1 ]
Wang, Haiqin [2 ,3 ]
He, Hongwu [2 ,3 ]
机构：
[1] Sun Yat Sen Univ, State Key Lab Oncol S China, Ctr Canc, Guangzhou 510060, Guangdong, Peoples R China
[2] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China
[3] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 04期
基金：
中国国家自然科学基金;
关键词：
Synthesis; Antitumor activity; 1,3-Benzenedicarbonyl dithioureas; SUBSTITUTED ACYL(THIO)UREA; PYRIMIDINE-DERIVATIVES; THIOUREA DERIVATIVES; POTENT INHIBITORS; SERIES;
D O I：
10.1016/j.bmcl.2010.12.130
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and biological activity of 1,3-benzenedicarbonyl dithioureas are described. Bioassay results indicated that these compounds exhibited cytotoxicity against various cancer cells. For example, compounds 4a showed the best inhibition activities against KB and CNE2 with IC50 10.72 and 9.91 mu M, respectively. (c) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1102 / 1104
页数：3
相关论文
共 15 条
  • [1] Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases
    Claridge, Stephen
    Raeppel, Franck
    Granger, Marie-Claude
    Bernstein, Naomy
    Saavedra, Oscar
    Zhan, Lijie
    Llewellyn, David
    Wahhab, Amal
    Deziel, Robert
    Rahil, Jubrail
    Beaulieu, Normand
    Nguyen, Hannah
    Dupont, Isabelle
    Barsalou, Annie
    Beaulieu, Carole
    Chute, Ian
    Gravel, Serge
    Robert, Marie-France
    Lefebvre, Sylvain
    Dubay, Marja
    Pascal, Roussen
    Gillespie, Jeff
    Jin, Zhiyun
    Wang, James
    Besterman, Jeffrey M.
    MacLeod, A. Robert
    Vaisburg, Arkadii
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (09) : 2793 - 2798
  • [2] [段志芳 Duan Zhifang], 2003, [应用化学, Chinese Journal of Applied Chemistry], V20, P80
  • [3] Identification of potent and selective inhibitors of PDGF receptor autophosphorylation
    Furuta, T
    Sakai, T
    Senga, T
    Osawa, T
    Kubo, K
    Shimizu, T
    Suzuki, R
    Yoshino, T
    Endo, M
    Miwa, A
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (07) : 2186 - 2192
  • [4] Biological activities studies and phase transfer catalysts promoting the one-pot synthesis of N-aryl-N′-(4-ethyloxy benzoyl)-thiourea derivatives
    Hu, Jing-Han
    Wang, Liang-Cheng
    Liu, Hong
    Wei, Tai-Bao
    [J]. PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2006, 181 (12) : 2691 - 2698
  • [5] Synthesis and herbicidal activity of N-(o-fluorophenoxyacetyl)thioureas derivatives and related fused heterocyclic compounds
    Ke, Shao-Yong
    Xue, Si-Jia
    [J]. ARKIVOC, 2006, : 63 - 68
  • [6] Peng H, 2007, CHINESE J ORG CHEM, V27, P502
  • [7] RANISE A, 1991, FARMACO, V46, P1203
  • [8] Ranise Angelo, 2003, Farmaco (Lausanne), V58, P765, DOI 10.1016/S0014-827X(03)00132-0
  • [9] Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase
    Sun, Chuanwen
    Zhang, Xiaodong
    Huang, Hai
    Zhou, Pei
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (24) : 8574 - 8581
  • [10] Molecular Docking and QSAR Studies on Substituted Acyl(thio)urea and Thiadiazolo [2,3-α] Pyrimidine Derivatives as Potent Inhibitors of Influenza Virus Neuraminidase
    Sun, Jiaying
    Cai, Shaoxi
    Mei, Hu
    Li, Jian
    Yan, Ning
    Wang, Qin
    Lin, Zhihua
    Huo, Danqun
    [J]. CHEMICAL BIOLOGY & DRUG DESIGN, 2010, 76 (03) : 245 - 254
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