TY - JOUR
T1 - Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents
AU - Mao, Shi Wei
AU - Chen, Huang
AU - Yu, Li Fang
AU - Lv, Fang
AU - Xing, Ya Jing
AU - Liu, Ting
AU - Xie, Jia
AU - Tang, Jie
AU - Yi, Zhengfang
AU - Yang, Fan
N1 - Publisher Copyright:
© 2016 Elsevier Masson SAS
PY - 2016
Y1 - 2016
N2 - A series of new seco-A ring bile acid diamides were synthesized, and their antiproliferative activities against PC3M (prostate), HT29 (colon) and ES-2 (ovarian) cancer cell lines were investigated using SRB assays. Most synthesized compounds presented improved antiproliferative activities compared to the parent bile acids (IC50> 80 μM), especially the piperazine conjugated compound 27 with IC50values of 1.07, 4.58 and 3.86 μM against PC3M, HT29 and ES-2 cancer cell lines, respectively. In addition, all the tested compounds showed less cytotoxic activity on a noncancerous cell line (HAF), and the most active compound 27 exhibited the highest selectivity (Selectivity Index, SIPC3M= 26.3). Furthermore, 27 could also enhance G1 arrest in PC3M cell, revealed by cell cycle analysis, and increase anti-migration activity on PC3M cells, confirmed by transwell migration assay.
AB - A series of new seco-A ring bile acid diamides were synthesized, and their antiproliferative activities against PC3M (prostate), HT29 (colon) and ES-2 (ovarian) cancer cell lines were investigated using SRB assays. Most synthesized compounds presented improved antiproliferative activities compared to the parent bile acids (IC50> 80 μM), especially the piperazine conjugated compound 27 with IC50values of 1.07, 4.58 and 3.86 μM against PC3M, HT29 and ES-2 cancer cell lines, respectively. In addition, all the tested compounds showed less cytotoxic activity on a noncancerous cell line (HAF), and the most active compound 27 exhibited the highest selectivity (Selectivity Index, SIPC3M= 26.3). Furthermore, 27 could also enhance G1 arrest in PC3M cell, revealed by cell cycle analysis, and increase anti-migration activity on PC3M cells, confirmed by transwell migration assay.
KW - Anticancer
KW - Antiproliferative activity
KW - Cell cycle arrest
KW - Migration
KW - Seco A-ring bile acid diamide
KW - Selectivity
UR - https://www.scopus.com/pages/publications/84978492650
U2 - 10.1016/j.ejmech.2016.04.055
DO - 10.1016/j.ejmech.2016.04.055
M3 - 文章
C2 - 27448915
AN - SCOPUS:84978492650
SN - 0223-5234
VL - 122
SP - 574
EP - 583
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -
