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1-Arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as Potent Histone Deacetylase Inhibitors Suppressing the Growth of Prostate Cancer Cells

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1-Arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as Potent Histone Deacetylase Inhibitors Suppressing the Growth of Prostate Cancer Cells

Yi-Min Liu et al. Eur J Med Chem.

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 N(1)-hydroxy-N(8)-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.

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