TY - JOUR
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
N1 - Publisher Copyright:
© 2014 Published by Elsevier Masson SAS.
PY - 2015/1
Y1 - 2015/1
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
UR - http://www.scopus.com/inward/record.url?scp=84908277134&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84908277134&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2014.10.052
DO - 10.1016/j.ejmech.2014.10.052
M3 - Article
C2 - 25462248
AN - SCOPUS:84908277134
SN - 0223-5234
VL - 89
SP - 320
EP - 330
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -
