Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs

  • Amal Mahmoud Youssef MoustafaEmail author
  • Safyah B. Bakare


A new series of hybrid 2-Quinolinone derivatives were synthesized and structurally proved using spectral and elemental analyses data. All the prepared compounds were tested for their in vitro cytotoxic activity against MCF-7 cell line. Compounds 6 and 8 showed potent anticancer activity, which were comparable to Doxorubicin as reference compound. While compound 3 was comparable to cisplatin. Cell cycle analysis of compounds 6 and 8 showed cell cycle arrest at S and G2/M phases of the cycle and induced apoptosis at pre-G1 phase. DNA synthesis inhibitory activity demonstrated that compound 6 showed equipotent activity to Doxorubicin. The extent of apoptosis was also determined using Annexin V-FITC assay. In addition, compounds 6 and 8 increase the activation of effector caspase 3 by four fold more than untreated control. On the other hand, the localization of compounds 3, 6 and 8 were found in the nucleus.


Mass spectrometry (MS) Infrared (IR) spectroscopy Cancer Cell line 


Supplementary material

11164_2019_3827_MOESM1_ESM.docx (323 kb)
Supplementary material 1 (DOCX 323 kb)


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Copyright information

© Springer Nature B.V. 2019

Authors and Affiliations

  • Amal Mahmoud Youssef Moustafa
    • 1
    Email author
  • Safyah B. Bakare
    • 2
  1. 1.Chemistry Department, Faculty of SciencePort Said UniversityPort SaidEgypt
  2. 2.Faculty of EducationShaqra UniversityAlmuzahimiyahKingdom of Saudi Arabia

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