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Design, Synthesis, and Anticancer Activity of New Quinazoline Derivatives as VEGFR-2 Inhibitors and Apoptosis Inducers

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Abstract

A new series of thiourea or thioacetamide linked quinazoline derivatives has been synthesized and tested for cytotoxicity against the HCT116 and MCF-7 cell lines. Compound 10b, demonstrates strong antiproliferative effect against both colon HCT-116 and MCF-7 cell lines. Compound 10b interrupts the HCT-116 cell cycle at the G2/M phase. According to DNA flow cytometry and annexin test, hybrid 10b is also capable of inducing cell cycle disruption and apoptosis in HCT-116 cells. It causes apoptosis by activating caspases-3, increasing proapoptotic Bax and p53 levels, and decreasing Bcl-2 protein levels. As a result, the novel derivative 10b may be regarded as a promising lead to antitumor agents development.

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ACKNOWLEDGMENTS

The authors are grateful to Taif University Deanship of Scientific research for Supporting Project number (20214), 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, Eman Y. Santali & Reem I. Alsantali

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  1. Marwa F. Ahmed
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  2. Eman Y. Santali
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  3. Reem I. Alsantali
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Correspondence to Marwa F. Ahmed.

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Ahmed, M.F., Santali, E.Y. & Alsantali, R.I. Design, Synthesis, and Anticancer Activity of New Quinazoline Derivatives as VEGFR-2 Inhibitors and Apoptosis Inducers. Russ J Gen Chem 92, 2047–2057 (2022). https://doi.org/10.1134/S107036322210019X

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