2. Academic Validation
  3. Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents

Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents

  • Eur J Med Chem. 2019 Apr 15:168:1-10. doi: 10.1016/j.ejmech.2019.02.033.
K Lakshmithendral 1,  K Saravanan 1,  R Elancheran 1,  K Archana 1,  N Manikandan 2,  H A Arjun 1,  M Ramanathan 2,  N K Lokanath 3,  S Kabilan 4
Affiliations

Affiliations

  • 1 Drug Discovery Lab, Department of Chemistry, Annamalai University, Annamalai Nagar, 608002, Tamil Nadu, India.
  • 2 Department of Pharmacology, PSG College of Pharmacy, Coimbatore, 641004, Tamil Nadu, India.
  • 3 Department of Studies in Physics, University of Mysore, Manasagangotri, Mysuru, 570 006, India.
  • 4 Drug Discovery Lab, Department of Chemistry, Annamalai University, Annamalai Nagar, 608002, Tamil Nadu, India. Electronic address: profdrskabilanau@gmail.com.
PMID: 30798049 DOI: 10.1016/j.ejmech.2019.02.033
Abstract

Structural based molecular docking approach revealed the findings of 2-(phenoxymethyl) -5-phenyl-1,3,4-oxadiazole derivatives. The compounds (7a-o) were synthesized and characterized well by using conventional methods. The compounds, 7b and 7m were reconfirmed through single crystal XRD analysis. The synthesized compounds (7a-o) were evaluated their antiproliferative activities against MCF-7 and MDA-MB-453. Furthermore, Lipinski's rule of five and pharmacokinetic properties were predicted for the test compounds. These results demonstrate that the compounds 7b and 7d exhibit more potent cytotoxicity and 7d exhibits dose-dependent activity and reduced cell viability. Further, the mechanism of action for the induced Apoptosis was observed through morphological changes and western blotting analysis. These findings may furnish the lead for further development.

Keywords

1,3,4-Oxadiazoles; Breast cancer; Estrogen receptor; Molecular docking.

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