Synthesis of a new class of furo[3,2-c]coumarins and its anticancer activity

J Photochem Photobiol B. 2015 Jul:148:66-72. doi: 10.1016/j.jphotobiol.2015.03.027. Epub 2015 Apr 3.

Abstract

A series of furo[3,2-c]coumarin derivatives 1a-d were synthesized and evaluated for their antiproliferative activity against MCF-7 breast and HCT-15 colon cancer cell lines using Sulfo-rhodamine B (SRB) assay. Compounds 1b and 1d showed higher antiproliferative activity than 1a and 1c. UV-Vis spectroscopy was used for DNA and BSA-binding affinity of the compounds 1b and 1d and gave overall affinity constants of K1b-DNA=8.1×10(3) M(-1), K1d-DNA=1.1×10(4) M(-1), K1b-BSA=5.1×10(4) M(-1), and K1d-BSA=7.6×10(4) M(-1). Our findings could provide new evidence showing the relationship between the chemical structure and anticancer activity of these new coumarin analogs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology
  • Binding Sites
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Coumarins / chemistry*
  • Coumarins / metabolism
  • Coumarins / pharmacology
  • DNA / chemistry
  • DNA / metabolism
  • Humans
  • Kinetics
  • MCF-7 Cells
  • Molecular Docking Simulation
  • Protein Binding
  • Protein Structure, Tertiary
  • Serum Albumin, Bovine / chemistry
  • Serum Albumin, Bovine / metabolism

Substances

  • Antineoplastic Agents
  • Coumarins
  • Serum Albumin, Bovine
  • DNA
  • coumarin