Synthesis and biological evaluation of a novel class of coumarin derivatives

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5274-8. doi: 10.1016/j.bmcl.2014.09.051.
Hong Li  1 ,  Xiaomin Wang  2 ,  Guichao Xu  1 ,  Li Zeng  1 ,  Kai Cheng  1 ,  Pengchao Gao  3 ,  Qing Sun  1 ,  Wei Liao  1 ,  Jianwei Zhang  4
Affiliations
  • 1. College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
  • 2. Department of Physiology, Key Laboratory for Neurodegenerative Disorders of the Ministry of Education, Capital Medical University, Beijing 100069, PR China.
  • 3. School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
  • 4. College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China. Electronic address: [email protected].
PMID: 25304898 DOI: 10.1016/j.bmcl.2014.09.051
Abstract

In this study, several novel coumarin derivatives, 7-hydroxy-2-oxo-2H-chromene-3-carboxyl-Trp-Trp-AA-OBzl compounds, were designed and synthesized as potential Anticancer agents. Their in vitro cytotoxic activities were evaluated using methylthiazoltetrazolium (MTT) assay. The anti-tumor activity of the newly coumarin derivatives was determined in a S180 bearing mouse model and some of the compounds demonstrated tumor growth inhibition similar to the positive control, doxorubicin. Compared to doxorubicin, most of the compounds exhibited enhanced immunologic function suggesting a relatively minor toxic effect. The intercalation of the coumarin derivatives synthesized with calf thymus (CT) DNA was also studied.

Keywords
Amino acid; Anti-tumor; Coumarin; Cytotoxicity; Peptide.