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Design, Synthesis, and Anticancer Activity of New Derivatives of Thiazole and Imidazole

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Abstract

A number of nitrogen heterocyclic derivatives, namely 1,3-thiazole and imidazolidine-2-thione, have been synthesized and their structures confirmed by IR, 1H and 13C NMR, and mass spectra. Cytotoxic activity of some synthesized products has been tested against human hepatocellular carcinoma (HepG2) cell line using the MTT assay. The most potent anti-proliferative agent demonstrates activity 2-fold higher than the reference compound doxorubicin. Three compounds have been characterized by IC50 value against VEGFR-2. The cell cycle analysis of compound 6 has demonstrated cell cycle arrest at G1 phase and accumulation of cells in pre-G1 phase indicating that cytotoxic activity proceeds via apoptotic pathway.

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Authors and Affiliations

  1. Chemistry Department, Faculty of Science, Port Said University, 42522, Port Said, Egypt

    I. M. El-Deen, E. H. Elsayed & M. S. Abd El-Azez

  2. Chemistry Department, Faculty of Science, Zagazig University, 44519, Zagazig, Egypt

    M. El-Ahwany

Authors
  1. I. M. El-Deen
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  2. E. H. Elsayed
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  3. M. El-Ahwany
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  4. M. S. Abd El-Azez
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Correspondence to M. S. Abd El-Azez.

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El-Deen, I.M., Elsayed, E.H., El-Ahwany, M. et al. Design, Synthesis, and Anticancer Activity of New Derivatives of Thiazole and Imidazole. Russ J Gen Chem 90, 2350–2355 (2020). https://doi.org/10.1134/S1070363220120191

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  • DOI: https://doi.org/10.1134/S1070363220120191

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