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

Jang-Yang Chang, Mei-Jung Lai, Yi-Ting Chang, Hsueh Yun Lee, Yun-Ching Cheng, Ching-Chuan Kuo, Min-Chieh Su, Chi-Yen Chang, Jing Ping Liou

Research output: Contribution to journalArticle

19 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)152-155
Number of pages4
JournalMedChemComm
Volume1
Issue number2
DOIs
Publication statusPublished - Aug 2010

Fingerprint

Tubulin
Antineoplastic Agents
Inhibitory Concentration 50
Colchicine
Binding Sites
Polymerization
Cells
Cell Line
benzenesulfonamide
Neoplasms
fosbretabulin
indoline

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents. / Chang, Jang-Yang; Lai, Mei-Jung; Chang, Yi-Ting; Lee, Hsueh Yun; Cheng, Yun-Ching; Kuo, Ching-Chuan; Su, Min-Chieh; Chang, Chi-Yen; Liou, Jing Ping.

In: MedChemComm, Vol. 1, No. 2, 08.2010, p. 152-155.

Research output: Contribution to journalArticle

Chang, Jang-Yang ; Lai, Mei-Jung ; Chang, Yi-Ting ; Lee, Hsueh Yun ; Cheng, Yun-Ching ; Kuo, Ching-Chuan ; Su, Min-Chieh ; Chang, Chi-Yen ; Liou, Jing Ping. / Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents. In: MedChemComm. 2010 ; Vol. 1, No. 2. pp. 152-155.
@article{b7adbf069f0743c591d0f25f2efbf73d,
title = "Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents",
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.",
author = "Jang-Yang Chang and Mei-Jung Lai and Yi-Ting Chang and Lee, {Hsueh Yun} and Yun-Ching Cheng and Ching-Chuan Kuo and Min-Chieh Su and Chi-Yen Chang and Liou, {Jing Ping}",
year = "2010",
month = "8",
doi = "10.1039/c0md00052c",
language = "English",
volume = "1",
pages = "152--155",
journal = "MedChemComm",
issn = "2040-2503",
publisher = "Royal Society of Chemistry",
number = "2",

}

TY - JOUR

T1 - Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents

AU - Chang, Jang-Yang

AU - Lai, Mei-Jung

AU - Chang, Yi-Ting

AU - Lee, Hsueh Yun

AU - Cheng, Yun-Ching

AU - Kuo, Ching-Chuan

AU - Su, Min-Chieh

AU - Chang, Chi-Yen

AU - Liou, Jing Ping

PY - 2010/8

Y1 - 2010/8

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=79952514549&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=79952514549&partnerID=8YFLogxK

U2 - 10.1039/c0md00052c

DO - 10.1039/c0md00052c

M3 - Article

AN - SCOPUS:79952514549

VL - 1

SP - 152

EP - 155

JO - MedChemComm

JF - MedChemComm

SN - 2040-2503

IS - 2

ER -