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Synthesis and biological screening of a novel enaminone-grafted trithiocarbonate: a potential anticancer and antimicrobial agent
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-04-21 , DOI: 10.1007/s00044-020-02535-2
Yahia Nasser Mabkhot , Jamal M. A. Khaled , Mujeeb A. S. Sultan , Naiyf S. H. A. Alharbi , Hazem A. Ghabbour , Fahd A. Nasr , Abdulrhman Alsayari , Abdullatif Bin Muhsinah , Hamed Algarni , Yahya I. Asiri

A need exists to develop safe and efficacious medications to treat major diseases such as cancer and infectious diseases. In response to this need, we synthesized a novel enaminone, which structurally belongs to the trithiocarbonate class engrafted by an enaminone group. The anticancer and antimicrobial activities were evaluated by utilizing three different types of human cancer (MDA-MB-231, LoVo, and HepG2) and a wide field of microbes (G+ and G bacteria, yeast, and molds). The tested compound 3 exhibited moderate growth suppression activity versus all examined human tumor cells, with values of IC50 ranging from 35 to 45 µg/ml. Moreover, the antimicrobial effects of compound 3 were more profound against fungal pathogens than against bacterial pathogens (minimal inhibitory concentrations; fungi, 0.08–0.14 mg/ml; bacteria, 0.3–1.4 mg/ml). These findings lay the foundation for designing improved bioactive agents that could be utilized as anticancer and/or antimicrobial agents.

中文翻译:

新型烯胺酮接枝的三硫代碳酸酯的合成和生物筛选:潜在的抗癌和抗菌剂

需要开发安全有效的药物来治疗主要疾病,例如癌症和传染病。为响应这一需求,我们合成了一种新型的烯胺酮,其结构上属于烯胺酮基团接枝的三硫代碳酸酯类。(G的抗癌和抗微生物活性通过利用三种不同类型的人类癌症(MDA-MB-231,株LoVo,和HepG2)和微生物的宽视场的评价+和G -细菌,酵母和霉菌)。与所有检查的人类肿瘤细胞相比,受试化合物3表现出中等的生长抑制活性,IC 50值为35至45 µg / ml。此外,化合物3的抗菌作用对真菌病原体的抵抗力要强于对细菌病原体的抵抗力(最小抑菌浓度;真菌,0.08-0.14 mg / ml;细菌,0.3-1.4 mg / ml)。这些发现为设计改进的可用作抗癌和/或抗微生物剂的生物活性剂奠定了基础。
更新日期:2020-04-21
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