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Biological evaluation and pharmacophore modeling of some benzoxazoles and their possible metabolites

Fatma Zilifdar1, Egemen Foto1, Tugba Ertan-Bolelli2

  • 1Faculty of Science, Department of Molecular Biology, Hacettepe University, Ankara, Turkey.

Archiv Der Pharmazie
|January 24, 2018
PubMed

Insights

New benzoxazole derivatives show potent anticancer activity. These compounds selectively kill cancer cells (HeLa) over normal cells (L929), indicating promise as novel therapeutic agents.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Research

Background:

  • Benzoxazole derivatives are explored for their therapeutic potential.
  • Identifying selective anticancer agents is crucial for effective cancer treatment.
  • Understanding mechanisms of action enhances drug development.

Purpose of the Study:

  • To evaluate novel benzoxazole derivatives as anticancer agents.
  • To assess the in vitro anti-proliferative and genotoxic activities of these compounds.
  • To develop pharmacophore models for selective cytotoxicity.

Main Methods:

  • Screening of 21 benzoxazole derivatives and metabolites for anti-proliferative activity using the SRB assay.
  • Testing against cancerous (HeLa) and non-cancerous (L929) cell lines.
  • Evaluating genotoxicity using the alkaline comet assay.

Main Results:

  • 17 out of 21 compounds exhibited cytotoxic activity against HeLa cells.
  • Cytotoxicity was significantly higher (15-700 times) in HeLa cells compared to L929 cells.
  • Compounds X17 and XT3 demonstrated selective genotoxicity against HeLa cells, inducing DNA strand breaks without affecting L929 cells.

Conclusions:

  • Benzoxazole derivatives show promising selective anticancer properties.
  • The identified compounds are effective candidates for anticancer drug development due to their targeted genotoxicity.
  • Pharmacophore models aid in understanding and predicting selective cytotoxic activity.
Keywords:
SRB assayanticancer activitybenzoxazolecomet assaypharmacophore

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