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

Research output: Contribution to journal › Article › peer-review

80 Citations (Scopus)

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.

Original language	English
Pages (from-to)	4351-4355
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	14
DOIs	https://doi.org/10.1021/jm800150d
Publication status	Published - Jul 24 2008

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

SDG 3 Good Health and Well-being

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm800150d

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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",

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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 - https://www.scopus.com/pages/publications/47749140369

UR - https://www.scopus.com/pages/publications/47749140369#tab=citedBy

U2 - 10.1021/jm800150d

DO - 10.1021/jm800150d

M3 - Article

C2 - 18588280

AN - SCOPUS:47749140369

SN - 0022-2623

VL - 51

SP - 4351

EP - 4355

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 14

ER -

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

Abstract

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