Synthesis, cytotoxic activity, and computational analysis of N10-substituted acridone analogs

Rajesh Kumar, Malkeet Singh Bahia, Om Silakari

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


A series of twenty N10-substituted acridone derivatives were synthesized, tested for in vitro cytotoxic activity, and analyzed computationally to predict their multi-drug resistance (MDR) modulation potential. All synthesized N10-substituted acridone analogs were tested for their in vitro cytotoxic activity against human breast adenocarcinoma (MCF-7), human small cell lung carcinoma (A-549), human colon adenocarcinoma (HT-29), and human cervical epithelioid carcinoma (HeLa) cell lines by MTT assay. The compounds were observed to be inactive against the HT-29 cell line. Among the synthesized compounds, compound 14 showed good in vitro activity against MCF-7, A-549, and HeLa cancer cell lines in the low micromolar (μM) range as compared to other compounds. Additionally, in silico study was performed to check the multi-drug resistance modulator (MDR) effect of these compounds using docking simulations in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of molecules 6, 7, 13, 14, 19, and 20 in the active site of this protein and proposed their dual action, i.e., anti-cancer and MDR modulation.

Original languageEnglish
Pages (from-to)921-933
Number of pages13
JournalMedicinal Chemistry Research
Issue number3
StatePublished - Mar 2015
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2014 Springer Science+Business Media New York.


  • Acridone derivatives
  • Cytotoxicity
  • Docking analysis
  • MTT assay
  • Multi-drug resistance


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