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

26 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 - Aug 2010

UN SDGs

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

SDG 3 Good Health and Well-being

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

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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 = "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 = aug,

doi = "10.1039/c0md00052c",

language = "English",

volume = "1",

pages = "152--155",

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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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U2 - 10.1039/c0md00052c

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ER -

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

Abstract

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