Synergistic Effect of the Combination of Novel Suberoylanilide Hydroxamic Acid Derivatives with Cisplatin on Anti-proliferation of Human Cancer Cells

被引：3

作者：

Xie, Rui ^{[1
]}

Shi, Jinghua ^{[1
]}

Cheng, Chunhui ^{[1
]}

Yun, Fan ^{[1
]}

Liu, Xia ^{[1
]}

Tang, Pingwah ^{[1
]}

Wu, Xinying ^{[1
]}

Yang, Ming ^{[1
]}

Yuan, Qipeng ^{[1
]}

机构：

[1] Beijing Univ Chem Technol, Coll Life Sci & Technol, Med Chem Res Div, State Key Lab Chem Resource Engn, Beijing 100029, Peoples R China

来源：

MEDICINAL CHEMISTRY | 2016年 / 12卷 / 08期

基金：

美国国家科学基金会;

关键词：

Synergistic effect; anti-proliferation; SAHA-based inhibitors; Cisplatin; hydroxamic acids; HISTONE DEACETYLASE INHIBITORS; DRUG-COMBINATION; PHASE-II; QUANTITATION; ANTAGONISM; ACETYLASES; EXPRESSION; APOPTOSIS; SAHA;

D O I：

10.2174/1573406412666160404125551

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel, green, and atom-economical boric acid catalyzed direct amidation without the use of any coupling agents for the preparation of suberoylanilide hydroxamic acid (SAHA) and SAHA-based inhibitors targeting anti-proliferation of cancer cells is provided. The new SAHA-based inhibitor B123, when used alone, exhibited higher anti-proliferative activities than SAHA or Cisplatin against a number of human cancer cells. We have examined the effect of combination of these SAHA-based inhibitors with Cisplatin. We found synergistic effects of the combination of SAHA-based inhibitors with Cisplatin over a wide range of concentrations against human liver cancer cells HepG2 and two human lung cancer cell lines H1299 and H460. This synergism leads up to 8-fold of dose reduction for Cisplatin in the combination with our synthesized inhibitor B123 against H1299.

引用

页码：767 / 774

页数：8

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