4.0 Article

Discovery of New Quinazoline-Based Anticancer Agents as VEGFR-2 Inhibitors and Apoptosis Inducers

Journal

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
Volume 48, Issue 4, Pages 739-748

Publisher

MAIK NAUKA/INTERPERIODICA/SPRINGER
DOI: 10.1134/S1068162022040033

Keywords

quinazoline; isatin; antitumor; caspases 3; cell cycle; apoptosis

Funding

  1. Taif University, Taif, Saudi Arabia [TURSP-2020/123]

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This article investigates the activity of novel quinazoline compounds (Xb) designed and synthesized, focusing on their effects on cell cycle and apoptosis. The results show that (Xb) can stop cell cycle at G2/M phase and induce apoptosis. This effect may be achieved by downregulating the expression of anti-apoptotic protein Bcl-2 and upregulating the expression levels of BAX and caspases 3.
Novel quinazoline compounds have been designed and synthesized aiming to discover new anticancer agents. Additional study was carried out on the most powerful derivatives, (Xb). A cell cycle research indicated that (Xb) mostly stops the cell cycle in the G2/M phase. The Annexin V-FITC apoptosis assay revealed that (Xb) increased apoptosis when compared with the control. It also demonstrated decreased anti-apoptotic Bcl-2 protein expression and increased BAX and caspases 3 expression levels.

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