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新型合成的氨基甲硫基-呋喃-2-甲酰胺衍生物的抗菌活性和抗癌潜力。

Anti-Microbial Activity and Anti-Cancer Potential of Novel Synthesized Carbamothioyl-Furan-2-Carboxamide Derivatives.

机构信息

Department of Chemistry, Government College University Faisalabad, Faisalabad 38000, Pakistan.

Department of Chemistry, University of Sahiwal, Sahiwal 57000, Pakistan.

出版信息

Molecules. 2023 Jun 6;28(12):4583. doi: 10.3390/molecules28124583.

Abstract

A series of carbamothioyl-furan-2-carboxamide derivatives were synthesized using a one-pot strategy. Compounds were obtained in moderate to excellent yields (56-85%). Synthesized derivatives were evaluated for their anti-cancer (HepG2, Huh-7, and MCF-7 human cancer cell lines) and anti-microbial potential. Compound p-tolylcarbamothioyl)furan-2-carboxamide showed the highest anti-cancer activity at a concentration of 20 μg/mL against hepatocellular carcinoma, with a cell viability of 33.29%. All compounds showed significant anti-cancer activity against HepG2, Huh-7, and MCF-7, while indazole and 2,4-dinitrophenyl containing carboxamide derivatives were found to be less potent against all tested cell lines. Results were compared with the standard drug doxorubicin. Carboxamide derivatives possessing 2,4-dinitrophenyl showed significant inhibition against all bacterial and fungal strains with inhibition zones (I.Z) in the range of 9-17 and MICs were found to be 150.7-295 μg/mL. All carboxamide derivatives showed significant anti-fungal activity against all tested fungal strains. Gentamicin was used as the standard drug. The results showed that carbamothioyl-furan-2-carboxamide derivatives could be a potential source of anti-cancer and anti-microbial agents.

摘要

采用一锅法合成了一系列碳硫酰基呋喃-2-甲酰胺衍生物。以中等至优良的收率(56-85%)获得了化合物。对合成的衍生物进行了抗癌症(HepG2、Huh-7 和 MCF-7 人癌细胞系)和抗微生物的潜力评估。在 20μg/mL 的浓度下,对肝癌具有最高的抗癌活性,细胞活力为 33.29%的对甲苯碳硫酰基呋喃-2-甲酰胺显示出最高的抗癌活性。所有化合物对 HepG2、Huh-7 和 MCF-7 均表现出显著的抗癌活性,而含吲唑和 2,4-二硝基苯基的酰胺衍生物对所有测试的细胞系的活性较低。结果与标准药物阿霉素进行了比较。含 2,4-二硝基苯基的酰胺衍生物对所有测试的细菌和真菌菌株均显示出显著的抑制作用,抑菌圈(I.Z)范围为 9-17,MIC 值为 150.7-295μg/mL。所有酰胺衍生物对所有测试的真菌菌株均表现出显著的抗真菌活性。庆大霉素被用作标准药物。结果表明,碳硫酰基呋喃-2-甲酰胺衍生物可能是抗癌和抗菌药物的潜在来源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fce/10300966/fc49138fa099/molecules-28-04583-g001.jpg

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