SYNTHESIS AND BIOACTIVITY OF NOVEL COUMARIN DERIVATIVES

Authors

  • Sai-Yang Zhang Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
  • Dong-Jun Fu Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
  • Hui-Hui Sun Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
  • Xiao-Xin Yue Henan Medical College, Zhengzhou 450001
  • Ying-Chao Liu Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
  • Yan-Bing Zhang Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
  • Hong-Min Liu Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001

DOI:

https://doi.org/10.1007/3099

Keywords:

coumarin, anticancer activity, antimicrobial activity

Abstract

A series of novel coumarin derivatives were synthesized from commercially available chemical agents. All prepared compounds were evaluated for their in vitro antiproliferative activity against five selected human cancer cell lines (EC109, MGC-803, PC-3, MCF-7, and EC9706) and their in vitro antimicrobial activity against E. coli and M. albicans. 4-(3-Bromopropoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MGC-803 cell line (IC50 47.7 μM) and 7-(2-bromoethoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MCF-7 cell line (IC50 48.3 μM). The latter compound was also the most active against E. coli (MIC50 0.27 μg/ml).

Author Biography

Dong-Jun Fu, Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001

Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University

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Published

2016-06-17

Issue

Vol. 52 No. 6 (2016)

Section

Original Papers