Issue 2, 2010
From the journal:

MedChemComm

Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents†

Jang-Yang Chang,‡bc   Mei-Jung Lai,‡a   Yi-Ting Chang,a   Hsueh-Yun Lee,a   Yun-Ching Cheng,b   Ching-Chuan Kuo,b   Min-Chieh Su,a   Chi-Yen Changb  and  Jing-Ping Liou*a  

* Corresponding authors

a College of Pharmacy, Taipei Medical University, 250 Wu-Xin Street, Taipei 110, Taiwan, Republic of China
E-mail: jpl@tmu.edu.tw
Tel: +886-2-27361661 ext. 6130

b National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, Republic of China

c Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital, Tainan 704, Taiwan, Republic of China

Abstract

A series of 7-arylindoline-1-benzenesulfonamides were prepared and evaluated for anticancer activity. 7-(4′-Cyanophenyl)indoline-1-benzenesulfonamide 15 exhibited substantial antiproliferative activity with IC50 values ranging from 17–32 nM against a variety of human cancer cell lines, including MDR resistant line. Compound 15 (IC50 = 1.5 μM) also showed more potent inhibition of tubulin polymerization than 4a (combretastatin A-4, IC50 = 2.0 μM) and displayed strong binding to the colchicine binding site of the tubulin.

Graphical abstract: Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents

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Article information

DOI
https://doi.org/10.1039/C0MD00052C
Article type
Concise Article
Submitted
22 Apr 2010
Accepted
28 Apr 2010
First published
18 May 2010

Med. Chem. Commun., 2010,1, 152-155

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Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents

J. Chang, M. Lai, Y. Chang, H. Lee, Y. Cheng, C. Kuo, M. Su, C. Chang and J. Liou, Med. Chem. Commun., 2010, 1, 152 DOI: 10.1039/C0MD00052C

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