Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

Jing Ping Liou; Zi Yi Wu; Ching Chuan Kuo; Chi Yen Chang; Pei Yi Lu; Chi Ming Chen; Hsing Pang Hsieh; Jang Yang Chang

doi:10.1021/jm800150d

Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

Jing Ping Liou, Zi Yi Wu, Ching Chuan Kuo, Chi Yen Chang, Pei Yi Lu, Chi Ming Chen, Hsing Pang Hsieh, Jang Yang Chang

研究成果: 雜誌貢獻 › 文章 › 同行評審

68 引文斯高帕斯（Scopus）

摘要

1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC₅₀ of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC₅₀ of 0.3-5.4 nM in a set of human cancer cell lines.

原文	英語
頁（從 - 到）	4351-4355
頁數	5
期刊	Journal of Medicinal Chemistry
卷	51
發行號	14
DOIs	https://doi.org/10.1021/jm800150d
出版狀態	已發佈 - 7月 24 2008

ASJC Scopus subject areas

有機化學

UN SDG

此研究成果有助於以下永續發展目標

存取文件

10.1021/jm800150d

其它文件與鏈接

Link to publication in Scopus

引用此

@article{9c1de90c75d441eb88704108f2a22813,

title = "Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors",

abstract = "1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC50 of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC50 of 0.3-5.4 nM in a set of human cancer cell lines.",

author = "Liou, {Jing Ping} and Wu, {Zi Yi} and Kuo, {Ching Chuan} and Chang, {Chi Yen} and Lu, {Pei Yi} and Chen, {Chi Ming} and Hsieh, {Hsing Pang} and Chang, {Jang Yang}",

year = "2008",

month = jul,

day = "24",

doi = "10.1021/jm800150d",

language = "English",

volume = "51",

pages = "4351--4355",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "14",

}

TY - JOUR

T1 - Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

AU - Liou, Jing Ping

AU - Wu, Zi Yi

AU - Kuo, Ching Chuan

AU - Chang, Chi Yen

AU - Lu, Pei Yi

AU - Chen, Chi Ming

AU - Hsieh, Hsing Pang

AU - Chang, Jang Yang

PY - 2008/7/24

Y1 - 2008/7/24

N2 - 1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC50 of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC50 of 0.3-5.4 nM in a set of human cancer cell lines.

AB - 1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC50 of 0.9 and 0.6 μM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC50 of 0.3-5.4 nM in a set of human cancer cell lines.

UR - http://www.scopus.com/inward/record.url?scp=47749140369&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=47749140369&partnerID=8YFLogxK

U2 - 10.1021/jm800150d

DO - 10.1021/jm800150d

M3 - Article

C2 - 18588280

AN - SCOPUS:47749140369

VL - 51

SP - 4351

EP - 4355

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 14

ER -

Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

摘要

ASJC Scopus subject areas

UN SDG

存取文件

其它文件與鏈接

指紋

引用此