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Design, Synthesis, and Cytotoxic Screening of New Quinoline Derivatives over MCF-7 Breast Cancer Cell Line

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Abstract

VEGFR-2 inhibition represents an attractive strategy for anticancer drug design. A new series of quinoline derivatives were synthesized and structurally confirmed with different spectroscopic techniques. VEGFR-2 inhibition assay showed that 2-(4-bromoquinolin-3-yloxy)-1-(4-chlorophenyl)ethanone (V) demonstrated potent VEGFR-2 inhibitory activities. In addition, the brominated quinoline (V) exhibit antitumor activity over MCF-7 cell line via cell cycle arrest at G1 phase and apoptosis inducing activity as revealed by cell cycle analysis and Annexin V/FITC staining assays. Moreover, brominated quinoline (V) was proved to upregulate expression of proteins that trigger apoptosis such as increased Bax, decreased Bcl-2 as well as increased Bax/Bcl-2 ratio.

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Authors and Affiliations

  1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, 42526, Egypt

    Islam Zaki

  2. Chemistry Department, Faculty of Science and Arts, Gurayat, Jouf University, Al-Jawf, 75911, Saudi Arabia

    Amal M. Imam

  3. Chemistry Department, Faculty of Science, Suez Canal University, Ismailia, 41522, Egypt

    Amal M. Imam

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  1. Islam Zaki
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Correspondence to Islam Zaki.

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Islam Zaki, Amal M. Imam Design, Synthesis, and Cytotoxic Screening of New Quinoline Derivatives over MCF-7 Breast Cancer Cell Line. Russ J Bioorg Chem 46, 1099–1109 (2020). https://doi.org/10.1134/S1068162020060096

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