Synthesis, cytotoxic study and docking based multidrug resistance modulator potential analysis of 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamides

Rajesh Kumar, Maninder Kaur, Malkeet Singh Bahia, Om Silakari

Research output: Contribution to journalArticlepeer-review

33 Scopus citations

Abstract

The present study describes the synthesis of fifteen 2-(9-oxoacridin-10(9H) -yl)-N-phenyl acetamide derivatives (13a-o) through condensation of 2-chloro-N-phenyl acetamides (12a-o) with acridone molecule (10). All the synthesized compounds were screened for their anti-cancer activity against three diverse cell lines including breast (MCF-7), cervical (HeLa) and lung adenocarcinoma (A-549) employing standard MTT assay. Among synthesized molecules, 13k and 13l showed good cytotoxicity activity against considered three cancer cell lines. Additionally, in silico studies of multidrug resistance modulator (MDR) effects of these compounds was performed by docking simulation in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of these molecules in the active site of this protein and predicted their MDR modulator behavior.

Original languageEnglish
Pages (from-to)83-91
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume80
DOIs
StatePublished - 10 Jun 2014
Externally publishedYes

Keywords

  • Acridone derivatives
  • Cytotoxicity
  • Docking analysis
  • MTT assay
  • Multidrug resistance

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