Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents

Shi Wei Mao; Huang Chen; Li Fang Yu; Fang Lv; Ya Jing Xing; Ting Liu; Jia Xie; Jie Tang; Zhengfang Yi; Fan Yang

doi:10.1016/j.ejmech.2016.04.055

Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents

Shi Wei Mao
, Huang Chen
, Li Fang Yu
, Fang Lv
, Ya Jing Xing
, Ting Liu
, Jia Xie
, Jie Tang
, Zhengfang Yi
, Fan Yang^*

^*Corresponding author for this work

East China Normal University

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

11 Citations (Scopus)

Abstract

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, SI^PC3M= 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.

Original language	English
Pages (from-to)	574-583
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	122
DOIs	https://doi.org/10.1016/j.ejmech.2016.04.055
Publication status	Published - 2016
Externally published	Yes

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Anticancer
Antiproliferative activity
Cell cycle arrest
Migration
Seco A-ring bile acid diamide
Selectivity

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10.1016/j.ejmech.2016.04.055

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@article{9d66bcf2c20947c18d9c6bc2fd09da36,

title = "Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents",

abstract = "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.",

keywords = "Anticancer, Antiproliferative activity, Cell cycle arrest, Migration, Seco A-ring bile acid diamide, Selectivity",

author = "Mao, \{Shi Wei\} and Huang Chen and Yu, \{Li Fang\} and Fang Lv and Xing, \{Ya Jing\} and Ting Liu and Jia Xie and Jie Tang and Zhengfang Yi and Fan Yang",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Masson SAS",

year = "2016",

doi = "10.1016/j.ejmech.2016.04.055",

language = "English",

volume = "122",

pages = "574--583",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

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

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 - Article

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 -

Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents

Abstract

UN SDGs

Keywords

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