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Synthesis and Cytotoxicity Screening of Some Synthesized Coumarin and Aza-Coumarin Derivatives as Anticancer Agents

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Abstract

A series of coumarin and aza-coumarin derivatives (II–IX) were synthesized and identified using IR, 1H NMR, and 13C NMR spectral data. All the synthesized compounds were assessed for their in vitro antiproliferative activity against Hepatocellular carcinoma (HepG2 cell line), and breast cancer (MCF-7 cell line). In vitro results showed that compounds (III) and (IX) were the most effective compounds against MCF-7 cell line and compound (IV) was the most effective compound against HepG2. Further in vitro study of compounds (III and IX). Compound (III) arrested cell cycle at G2/M phase and induction of apoptosis at pre-G1 phase while compound (IX) arrested cell cycle at G1/S phase. The most potent compounds (III and IX) showed good inhibitory activity against topoisomerase II enzyme. Also, compounds (III and IX) have induced apoptosis at the early and late apoptotic levels.

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Authors and Affiliations

  1. Department of Chemistry, Faculty of Science, Port Said University, Port Said, 42526, Egypt

    Ibrahim M. El-Deen, Manar A. El-Zend & Lamiaa A. A. Barakat

  2. Medical Research Division, National Research Centre, Dokki, Giza, 12622, Egypt

    Mohamed A. Tantawy

Authors
  1. Ibrahim M. El-Deen
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  2. Manar A. El-Zend
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  3. Mohamed A. Tantawy
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  4. Lamiaa A. A. Barakat
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Correspondence to Manar A. El-Zend.

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Ibrahim M. El-Deen, El-Zend, M.A., Tantawy, M.A. et al. Synthesis and Cytotoxicity Screening of Some Synthesized Coumarin and Aza-Coumarin Derivatives as Anticancer Agents. Russ J Bioorg Chem 48, 380–390 (2022). https://doi.org/10.1134/S106816202202011X

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