Synthesis and docking studies on styryl chromones exhibiting cytotoxicity in human breast cancer cell line

被引:17
作者
Bhatnagar, Seema [1 ]
Sahi, Shakti [2 ]
Kackar, Puneet [3 ,4 ]
Kaushik, Swati [1 ]
Dave, Manan K. [1 ]
Shukla, Akshara [1 ]
Goel, Ashita [1 ]
机构
[1] Amity Univ Sector 125, Amity Inst Biotechnol, Chem Synth Grp, Noida, India
[2] Gautam Buddha Univ, Sch Biotechnol, Greater Noida 201308, India
[3] Amity Univ Sector 125, Amity Inst Biotechnol, Bioinformat Grp, Noida, India
[4] Italian Inst Technol, Cent Res Labs Genoa Headquarter, Unit Drug Discovery & Dev, I-16163 Genoa, Italy
关键词
Estrogen receptor; Styryl chromones; ESTROGEN-RECEPTOR;
D O I
10.1016/j.bmcl.2010.05.108
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The search for small molecules that preferentially target the functionally important surfaces of estrogen receptor and disrupt the transcriptional activity in the cell has emerged as a promising area towards rationale based drug design. Herein, we report substituted styryl chromones as a new class of compounds that exhibit selectivity for ER beta binding at the second binding site of HT and antiproliferative activity in human breast cancer cell line. (c) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4945 / 4950
页数:6
相关论文
共 10 条
  • [1] Eicher T., 2003, CHEMISTRYOFHETEROCYC, P257
  • [2] Phototransformations of some 3-alkoxy-2-styrylchromones: type II cyclisations of 1,4-and 1,6-biradicals
    Gupta, SC
    Yusuf, M
    Sharma, S
    Saini, A
    Arora, S
    Kamboj, RC
    [J]. TETRAHEDRON, 2004, 60 (38) : 8445 - 8454
  • [3] A two-site model for antiestrogen action
    Jensen, EV
    Khan, SA
    [J]. MECHANISMS OF AGEING AND DEVELOPMENT, 2004, 125 (10-11) : 679 - 682
  • [4] Maggiolini M, 2001, MOL PHARMACOL, V60, P595
  • [5] Benzopyrans as selective estrogen receptor β agonists (SERBAs).: Part 2:: Structure-activity relationship studies on the benzopyran scaffold
    Richardson, Timothy I.
    Norman, Bryan H.
    Lugar, Charles W.
    Jones, Scott A.
    Wang, Yong
    Durbin, Jim D.
    Krishnan, Venkatesh
    Dodge, Jeffrey A.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (13) : 3570 - 3574
  • [6] Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor a coactivator binding
    Rodriguez, AL
    Tamrazi, A
    Collins, ML
    Katzenellenbogen, JA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (03) : 600 - 611
  • [7] *SCHROD, SCHROD SUIT 2008
  • [8] The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
    Shiau, AK
    Barstad, D
    Loria, PM
    Cheng, L
    Kushner, PJ
    Agard, DA
    Greene, GL
    [J]. CELL, 1998, 95 (07) : 927 - 937
  • [9] Synthesis and reactivity of styrylchromones
    Silva, AMS
    Pinto, DCGA
    Cavaleiro, JAS
    Levai, A
    Patonay, T
    [J]. ARKIVOC, 2004, : 106 - 123
  • [10] A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor β
    Wang, Yong
    Chirgadze, Nickolay Y.
    Briggs, Stephen L.
    Khan, Sohaib
    Jensen, Elwood V.
    Burris, Thomas P.
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2006, 103 (26) : 9908 - 9911