新型磺胺甲恶唑衍生物的合成及抗癌抗菌性能研究。
Synthesis of novel sulphamethoxazole derivatives and exploration of their anticancer and antimicrobial properties.
机构信息
Department of Organic Chemistry, Kaunas University of Technology, Kaunas, Lithuania.
Laboratory of Drug Targets Histopathology, Institute of Cardiology, Lithuanian University of Health Sciences, Kaunas, Lithuania.
出版信息
PLoS One. 2023 Mar 23;18(3):e0283289. doi: 10.1371/journal.pone.0283289. eCollection 2023.
A series of new derivatives based on sulfamethoxazole were designed and synthesized in this study. The structures of the new compounds were confirmed based on a comprehensive characterization of spectral data by applied IR and 1H as well as 13C NMR spectroscopy. The prepared compounds were tested for their anticancer and antimicrobial properties. Hydrazone 16b demonstrated convincing anticancer effect against all tested cell cultures such as human prostate carcinoma PPC-1 and human kidney carcinoma CaKi-1 cell lines, and human fibroblasts HF, n = 3. The most promising compound 16b showed higher activity against CaKi-1 cell line than the anticancer drugs axitinib and pazopanib used to treat renal cancer. Also, it was more active in the PPC-1 cell line compared to the approved PARP inhibitor Olaparib. Hydrazone 16b was also found to possess good antimicrobial properties against gram-positive bacteria strains of Staphylococcus aureus, Staphylococcus epidermidis, as well as Bacillus cereus.
本研究设计并合成了一系列基于磺胺甲恶唑的新衍生物。通过应用红外和 1H 以及 13C NMR 光谱对光谱数据进行综合表征，确定了新化合物的结构。测试了所制备的化合物的抗癌和抗菌性能。腙 16b 对所有测试的细胞培养物（如人前列腺癌细胞系 PPC-1 和人肾癌细胞系 CaKi-1 以及人成纤维细胞 HF）均表现出令人信服的抗癌作用，n = 3。最有前途的化合物 16b 对 CaKi-1 细胞系的活性高于用于治疗肾癌的抗癌药物阿昔替尼和帕唑帕尼。此外，与已批准的 PARP 抑制剂奥拉帕利相比，它在 PPC-1 细胞系中也更具活性。腙 16b 还对金黄色葡萄球菌、表皮葡萄球菌和蜡样芽孢杆菌等革兰氏阳性菌菌株具有良好的抗菌性能。
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