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    題名: Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents
    作者: Wang, Ruei‐Yu;Li, Cai‐Wei;Cho, Shu‐Tse;Chang, Chun‐Hao;Chen, Jih‐Jung;Shih, Tzenge‐Lien
    關鍵詞: cinnamil;pancreatic cancer;quinoxaline
    日期: 2022-05-02
    上傳時間: 2022-05-04 12:10:19 (UTC+8)
    出版者: Wiley-VCH Verlag GmbH & Co. KGaA
    摘要: 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.
    關聯: Archiv der Pharmazie 355(5), 2100448
    DOI: 10.1002/ardp.202100448
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