Synthesis and in vitro evaluation of novel coumarin-chalcone hybrids as potential anticancer agents

被引:259
作者
Sashidhara, Koneni V. [1 ]
Kumar, Abdhesh [1 ]
Kumar, Manoj [1 ]
Sarkar, Jayanta [2 ]
Sinha, Sudhir [2 ]
机构
[1] Cent Drug Res Inst CDRI CSIR, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst CDRI CSIR, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India
关键词
Synthesis; Coumarin; Chalcone; In vitro; Cytotoxicity; BIOLOGICAL EVALUATION; ANALOGS; DESIGN; DERIVATIVES;
D O I
10.1016/j.bmcl.2010.10.116
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of coumarin-chalcone hybrids have been synthesized and evaluated for their in vitro cytotoxicity against a panel of four human cancer cell lines and normal fibroblasts (NIH3T3). Among 21 compounds screened, three compounds (23, 25 and 26) showed IC50 range from 3.59 to 8.12 mu M. The most promising compound 26 showed around 30-fold more selectivity towards C33A (cervical carcinoma) cells over normal fibroblast NIH3T3 cells with an IC50 value of 3.59 mu M. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7205 / 7211
页数:7
相关论文
共 39 条
  • [1] Antimycobacterial Coumarins from the Sardinian giant fennel (Ferula communis)
    Appendino, G
    Mercalli, E
    Fuzzati, N
    Arnoldi, L
    Stavri, M
    Gibbons, S
    Ballero, M
    Maxia, A
    [J]. JOURNAL OF NATURAL PRODUCTS, 2004, 67 (12): : 2108 - 2110
  • [2] SYNTHESIS AND CYTOSTATIC ACTIVITY OF GEIPARVARIN ANALOGS
    BARALDI, PG
    GUARNERI, M
    MANFREDINI, S
    SIMONI, D
    BALZARINI, J
    DECLERCQ, E
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (02) : 284 - 288
  • [3] Design, synthesis and anticancer activities of stilbene-coumarin hybrid compounds: Identification of novel proapoptotic agents
    Belluti, Federica
    Fontana, Gabriele
    Dal Bo, Laura
    Carenini, Nives
    Giommarelli, Chiara
    Zunino, Franco
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 18 (10) : 3543 - 3550
  • [4] Bombardelli E., 2001, PCT Int. Pub. No, Patent No. [WO 01/17984 Al, 0117984]
  • [5] Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2′,5′-dialkoxylchalcones as cancer chemopreventive agents
    Cheng, Jen-Hao
    Hung, Chi-Feng
    Yang, Shyh-Chyun
    Wang, Jih-Pyang
    Won, Shen-Jeu
    Lin, Chun-Nan
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (15) : 7270 - 7276
  • [6] Mechanism-based target identification and drug discovery in cancer research
    Gibbs, JB
    [J]. SCIENCE, 2000, 287 (5460) : 1969 - 1973
  • [7] Chalcones: An update on cytotoxic and chemoprotective properties
    Go, ML
    Wu, X
    Liu, XL
    [J]. CURRENT MEDICINAL CHEMISTRY, 2005, 12 (04) : 483 - 499
  • [8] Pharmacological and biochemical actions of simple coumarins: Natural products with therapeutic potential
    Hoult, JRS
    Paya, M
    [J]. GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM, 1996, 27 (04): : 713 - 722
  • [9] Kennedy R. O., 1997, COUMARINS BIOL APPL
  • [10] Total synthesis of xanthohumol
    Khupse, Rahul S.
    Erhardt, Paul W.
    [J]. JOURNAL OF NATURAL PRODUCTS, 2007, 70 (09): : 1507 - 1509