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Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents

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We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2‐diaminobenzene. Among the 26 synthesized compounds reported in this… Click to show full abstract

We synthesized multiple cinnamils and quinoxalines to evaluate their anticancer activity. Cinnamils were used as precursors for quinoxalines via condensation with 1,2‐diaminobenzene. Among the 26 synthesized compounds reported in this article, we found that cinnamil 3l exhibited its inhibitory effect with an IC50 value of 1.45 ± 0.98 μM, significantly higher than doxorubicin (8.5 ± 0.85 μM) against pancreatic cancer cells (PANC‐1). Additionally, cinnamil 3l (IC50 10.98 ± 3.63 μM) showed less cytotoxicity than doxorubicin to Hs68 cells (0.92 ± 1.11 μM). The colony formation assay demonstrated that 3l obviously decreased the PANC‐1 cell viability, and Western blot assays confirmed that 3l markedly induced apoptosis of PANC‐1 cells through Bax, Bcl‐2, and caspase 3 signaling cascades. These results demonstrate that cinnamil 3l has great potential to be further developed as a promising chemotherapeutic agent for pancreatic cancer.

Keywords: cinnamils quinoxalines; quinoxalines biological; biological evaluation; synthesis cinnamils; evaluation anticancer; anticancer

Journal Title: Archiv der Pharmazie
Year Published: 2022

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