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Design, Synthesis, Anticancer Activity, and Cell Cycle Analysis of Novel Quinazoline Derivatives Targeting VEGFR-2 Kinase

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Abstract

Novel quinazoline derivatives have been designed, synthesized and tested for cytotoxic activity against HCT116, and MCF-7 cell lines. The preliminary data indicate their promising antitumor potential. Enzyme inhibitory activity of the most active product against VEGFR-2 has been assessed. Apoptosis and cell cycle arrest during the G2/M phase has been triggered by the product, and according to the gene expression data, it increases BAX and caspase-3 expression while decreasing Bcl-2 expression.

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ACKNOWLEDGMENTS

The authors are grateful to Taif University Researchers Supporting Project number (TURSP-2020/123), Taif University, Taif, Saudi Arabia, for their support.

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O. Box 11099, 21944, Taif, Saudi Arabia

    Marwa F. Ahmed

  2. Department of Pharmaceutics, College of Pharmacy, Taif University, P.O. Box 11099, 21944, Taif, Saudi Arabia

    Amany S. Khalifa

  3. Department of Clinical Laboratories Sciences, College of Applied Medical Sciences, Taif University, P.O. Box 11099, 21944, Taif, Saudi Arabia

    Emad M. Eed

Authors
  1. Marwa F. Ahmed
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  2. Amany S. Khalifa
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Correspondence to Marwa F. Ahmed.

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Ahmed, M.F., Khalifa, A.S. & Eed, E.M. Design, Synthesis, Anticancer Activity, and Cell Cycle Analysis of Novel Quinazoline Derivatives Targeting VEGFR-2 Kinase. Russ J Gen Chem 91, 2497–2505 (2021). https://doi.org/10.1134/S1070363221120203

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