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

doi:10.1039/c0md00052c

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 journal › Article › peer-review

24 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 language	English
Pages (from-to)	152-155
Number of pages	4
Journal	MedChemComm
Volume	1
Issue number	2
DOIs	https://doi.org/10.1039/c0md00052c
Publication status	Published - 2010 Aug

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1039/c0md00052c

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

year = "2010",

month = aug,

doi = "10.1039/c0md00052c",

language = "English",

volume = "1",

pages = "152--155",

journal = "MedChemComm",

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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.

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

Abstract

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