Modeling, design and synthesis of new heteroaryl ethylenes active against the MCF-7 breast cancer cell-line

Mol Biosyst. 2013 Oct;9(10):2426-9. doi: 10.1039/c3mb70151d.

Abstract

A dataset of 50 compounds was used to generate a QSAR model and to design 9 new heteroaryl ethylenes. These compounds were synthesized, tested in vitro and a significant agreement with in silico predictions observed. Studies using Laser Scanning Confocal Microscopy pointed out that the compounds may act by different mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Breast Neoplasms
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Ethylenes / chemical synthesis
  • Ethylenes / chemistry*
  • Ethylenes / pharmacology
  • Female
  • Humans
  • Inhibitory Concentration 50
  • MCF-7 Cells
  • Models, Molecular*
  • Quantitative Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Ethylenes