Design, Synthesis and Anti-breast Cancer Activity of Some Novel Substituted Isoxazoles as Anti-breast Cancer Agent

Anticancer Agents Med Chem. 2018;18(7):1009-1015. doi: 10.2174/1871520618666171129153655.

Abstract

Methods: A novel series of isoxazole (S21-S30) derivatives were designed, synthesized and screened for their anticancer activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. The synthesized derivative has the ability to inhibit the growth of the human breast cancer cell line at low concentrations. In vivo anticancer activity was performed on virgin female sprague dawley rats.

Results: The result shows that compound S23 has more selectivity and marked estrogen modulator activity than the standard tamoxifen.

Keywords: Chalcone; S21-S30; breast cancer; estrogen receptor; isoxazole; tamoxifen..

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Breast / drug effects
  • Breast / metabolism
  • Breast / pathology
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Design
  • Female
  • Humans
  • Isoxazoles / chemical synthesis
  • Isoxazoles / chemistry*
  • Isoxazoles / pharmacology
  • Isoxazoles / therapeutic use*
  • MCF-7 Cells
  • Molecular Docking Simulation
  • Rats, Sprague-Dawley
  • Receptors, Estrogen / metabolism

Substances

  • Antineoplastic Agents
  • Isoxazoles
  • Receptors, Estrogen