新型羟基吡喃酮的合成及其对不同细胞系细胞毒性的研究

Q4 Pharmacology, Toxicology and Pharmaceutics
Pelin Nur ÜÇKAN, Gülşah KARAKAYA, Beyza DÜZLEYEN, Canan SEVİMLİ GÜR, Mutlu AYTEMİR
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引用次数: 0

摘要

由曲酸合成的曼尼希碱在我们研究组进行的广泛研究中已经确定它们具有广泛的生物活性。& # x0D;本研究从具有高抗癌活性的化合物中合成了新的抗癌活性化合物。利用光谱学方法和元素分析鉴定了化合物的结构。用MTT法对不同的人癌细胞进行了细胞毒性筛选。 化合物1具有显著的细胞毒性,IC50值在8.11 ~ 21.24µg/mL之间。对Vero(非洲绿猴肾上皮)的IC50值大于100µg/mL,这意味着对健康细胞的细胞毒性低。与此相比,SK-MEL细胞的IC50值降低了12倍,治疗指数超过12。在SK-MEL细胞系上,化合物1的细胞毒活性比先前报道的细胞毒剂KOJI MG84的细胞毒活性低4倍,与KOJI MG84最接近。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and Investigation of Cytotoxicity in Different Cell Lines of Novel Hydroxypyranones
Mannich bases synthesized from kojic acid have been determined in extensive studies conducted by our study group that they have a wide variety of biological activities. In this study, new anticancer-active compounds were synthesized from compounds with high anticancer activity. The compounds' structures were identified through the utilization of spectroscopic methods and elemental analyses. The cytotoxicity screening of the compounds were done by MTT assay on different human cancer cell lines. Compound 1 bearing iodomethyl moiety, showed remarkable cytotoxicity with IC50 values in the range of 8.11 and 21.24 µg/mL. The IC50 value on Vero (African green monkey kidney epithelial) is over 100 µg/mL which means low cytotoxicity against healthy cells. Compared to this, SK-MEL cells have 12 times less IC50 value, with a therapeutic index over 12. The closest cytotoxic effectivity to KOJI MG84 which is previously reported as a cytotoxic agent, is observed on the SK-MEL cell line in compound 1, with 4 times less cytotoxic activity.
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来源期刊
Hacettepe University Journal of the Faculty of Pharmacy
Hacettepe University Journal of the Faculty of Pharmacy Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
0.60
自引率
0.00%
发文量
18
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