Preparation and biological evaluation of coumarin amide derivatives bearing fluorine as potential fungicides and anticancer agents

Xiang, Xin; Chen, Yafang; Wu, Lang; Zhang, Long; Zhang, Yan; Yang, Wude; Yu, Xiang

doi:10.1016/j.arabjc.2024.105872

Arabian Journal of Chemistry

2024

DOI: 10.1016/j.arabjc.2024.105872

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Preparation and biological evaluation of coumarin amide derivatives bearing fluorine as potential fungicides and anticancer agents

Xin Xiang,

Yafang Chen,

Lang Wu

et al.

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2024

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Natural Products‐Based Anticancer Agents: Synthesis and Anticancer Activities of Funtumine Amide/Sulfonamide Derivatives

Wu,

Xiang,

Zhang

et al. 2024

Chemistry & Biodiversity

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Funtumine is a pregnene‐type steroidal alkaloid exhibiting moderate anticancer activity. To discover novel natural product‐based anticancer drugs, a series of novel funtumine amide/sulfonamide derivatives were papered and identified using spectroscopic techniques. Additionally, the structures of compounds 2j, 3a, and 4k were further confirmed through X‐ray diffraction analysis. Biological activity experiments conducted against three cancer cell lines revealed that several of the synthesized compounds demonstrated inhibition activities comparable to or exceeding those of the commercial anticancer agent, 5‐Fluorouracil. Especially compound 4i demonstrated a notably strong growth inhibitory effect on HePG2 (IC50 = 14.89 μM) and HCT116 (IC50 = 15.67 μM) cell lines, while exhibiting minimal cytotoxicity towards human normal BEAS‐2B cells. Preliminary structure‐activity relationships (SARs) analysis indicated that the conversion of the carbonyl group at the C‐20 position of funtumine to a hydroxyl group could yield more potent compounds.

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Natural Products‐Based Anticancer Agents: Synthesis and Anticancer Activities of Funtumine Amide/Sulfonamide Derivatives

Wu,

Xiang,

Zhang

et al. 2024

Chemistry & Biodiversity

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show abstract

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Preparation and biological evaluation of coumarin amide derivatives bearing fluorine as potential fungicides and anticancer agents

Cited by 1 publication

References 48 publications

Natural Products‐Based Anticancer Agents: Synthesis and Anticancer Activities of Funtumine Amide/Sulfonamide Derivatives

Natural Products‐Based Anticancer Agents: Synthesis and Anticancer Activities of Funtumine Amide/Sulfonamide Derivatives

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