Synthesis and biological applications of some novel 8-Hydroxyquinoline urea and thiourea derivatives

Mohammad A. Khasawneh, Ayesha AlKaabi, Abdelouahid Samadi, Priya Antony, Ranjit Vijayan, Lamya Ahmed Al-Keridis, Haythem A. Saadeh, Nael Abutaha

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)


A number of novel urea and thiourea derivatives of 8-hydroxyquinoline have been designed, synthesized and evaluated for their anticancer activities. The structures of the new compounds were established by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry. The in vitro cytotoxicity against MCF7, and MDA-MB-231 cell lines were assessed by MTT assay. Six of the 11 compounds synthesized namely 5b, 5c, 5f, and 6b-d exhibited cytotoxicity with IC50 values ranged between 0.5 and 42.4 µM. Apoptotic features of cells treated with 5b compound were observed via florescent microscopy using DAPI and ethidium bromide/acridine orange staining against MCF-7 cells. Molecular docking of these molecules against 16 potential breast cancer protein revealed that these compounds could interact with the active site of poly (ADP-ribose) polymerase-1 (PARP1), B-cell lymphoma-extra large (Bcl-xL) and PARP5A (Tankyrase 1) by forming hydrogen bonds, π-π interactions and hydrophobic interactions. The docked poses of these molecules were observed to be similar in the active site of each of these targets.

Original languageEnglish
Article number103905
JournalArabian Journal of Chemistry
Issue number7
Publication statusPublished - Jul 2022


  • 8-Hydroxyquinoline
  • Anticancer
  • Apoptosis
  • Molecular Docking
  • Piperazine
  • Thiourea
  • Urea

ASJC Scopus subject areas

  • General Chemistry
  • General Chemical Engineering


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