1-arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as potent histone deacetylase inhibitors suppressing the growth of prostate cancer cells

Yi-Min Liu, Hsueh Yun Lee, Chun-Han Chen, Chia-Hua Lee, Li-Ting Wang, Shiow Lin Pan, Mei-Jung Lai, Teng-Kuang Yeh, Jing Ping Liou

研究成果: 雜誌貢獻文章

13 引文 (Scopus)

摘要

This study describes the development of a series of 1-arylsulfonyl-6-(N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)acrylamide (11) exhibits marked anti-HDAC and antiproliferative activity, and is slightly more effective than N1-hydroxy-N8-phenyloctanediamide (SAHA, Vorinostat, 1). In a xenograft tumor model, 11, at doses of 100 or 200 mg/kg orally, suppresses the growth of PC-3 cells and leads to tumor growth inhibition of 38.8% and 57.9%, respectively. Compound 11 is a lead compound for further development of potential prostate cancer inhibitors.
原文英語
頁(從 - 到)320-330
頁數11
期刊European Journal of Medicinal Chemistry
89
DOIs
出版狀態已發佈 - 2015

指紋

Histone Deacetylase Inhibitors
Tumors
Prostatic Neoplasms
Cells
Lead compounds
Histone Deacetylases
Acrylamide
Growth
Heterografts
Neoplasms
1,2,3,4-tetrahydroquinoline
vorinostat
Lead

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology
  • Medicine(all)

引用此文

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title = "1-arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as potent histone deacetylase inhibitors suppressing the growth of prostate cancer cells",
abstract = "This study describes the development of a series of 1-arylsulfonyl-6-(N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)acrylamide (11) exhibits marked anti-HDAC and antiproliferative activity, and is slightly more effective than N1-hydroxy-N8-phenyloctanediamide (SAHA, Vorinostat, 1). In a xenograft tumor model, 11, at doses of 100 or 200 mg/kg orally, suppresses the growth of PC-3 cells and leads to tumor growth inhibition of 38.8{\%} and 57.9{\%}, respectively. Compound 11 is a lead compound for further development of potential prostate cancer inhibitors.",
keywords = "Histone deacetylase inhibitors, Prostate cancer, Quinoline",
author = "Yi-Min Liu and Lee, {Hsueh Yun} and Chun-Han Chen and Chia-Hua Lee and Li-Ting Wang and Pan, {Shiow Lin} and Mei-Jung Lai and Teng-Kuang Yeh and Liou, {Jing Ping}",
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T1 - 1-arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as potent histone deacetylase inhibitors suppressing the growth of prostate cancer cells

AU - Liu, Yi-Min

AU - Lee, Hsueh Yun

AU - Chen, Chun-Han

AU - Lee, Chia-Hua

AU - Wang, Li-Ting

AU - Pan, Shiow Lin

AU - Lai, Mei-Jung

AU - Yeh, Teng-Kuang

AU - Liou, Jing Ping

PY - 2015

Y1 - 2015

N2 - This study describes the development of a series of 1-arylsulfonyl-6-(N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)acrylamide (11) exhibits marked anti-HDAC and antiproliferative activity, and is slightly more effective than N1-hydroxy-N8-phenyloctanediamide (SAHA, Vorinostat, 1). In a xenograft tumor model, 11, at doses of 100 or 200 mg/kg orally, suppresses the growth of PC-3 cells and leads to tumor growth inhibition of 38.8% and 57.9%, respectively. Compound 11 is a lead compound for further development of potential prostate cancer inhibitors.

AB - This study describes the development of a series of 1-arylsulfonyl-6-(N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)acrylamide (11) exhibits marked anti-HDAC and antiproliferative activity, and is slightly more effective than N1-hydroxy-N8-phenyloctanediamide (SAHA, Vorinostat, 1). In a xenograft tumor model, 11, at doses of 100 or 200 mg/kg orally, suppresses the growth of PC-3 cells and leads to tumor growth inhibition of 38.8% and 57.9%, respectively. Compound 11 is a lead compound for further development of potential prostate cancer inhibitors.

KW - Histone deacetylase inhibitors

KW - Prostate cancer

KW - Quinoline

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U2 - 10.1016/j.ejmech.2014.10.052

DO - 10.1016/j.ejmech.2014.10.052

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VL - 89

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EP - 330

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

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