新型甾体杂环化合物的合成及细胞毒活性评价。
Synthesis and cytotoxic evaluation of novel hybrid estrane heterocycles as chemotherapeutic anti-cancer agents.
机构信息
Department of Chemistry, Faculty of Science, Menofia University, Shebin El-Koam, Egypt.
Hormones Department, National Research Centre, 12622 Dokki, Giza, Egypt.
出版信息
Steroids. 2021 May;169:108813. doi: 10.1016/j.steroids.2021.108813. Epub 2021 Feb 27.
New synthesized hybrid steroidal heterocyclic compounds have received a lot of attention in view of their biological activities as anticancer agents. In this study, a novel class of hybrid estrane heterocyclic compounds were synthesized and evaluated by analytical and spectral data which proved the validity of these derivatives. The cytotoxicity of synthesized compounds 2a, 2b, 2c, 3b, 8, 10a, 10b, 13, 14, 16a and 19 against three human cell lines: breast cancer cells (MCF-7), prostate cancer cells (PC3), and liver cancer cells (HepG2) has been tested using MTT assay. Compounds 10a, 10b, 2c, and 14 revealed more inhibitory influence on MCF7, PC3 and HepG2 growth than the reference drug doxorubicin (Dox) after 24 h incubation. Noteworthy, the tested compounds 10a, 10b, 2c, and 14 exhibited the most pronounced effect in this respect. The results were confirmed by morphology study.
新型合成甾体杂环化合物因其作为抗癌剂的生物活性而受到广泛关注。在这项研究中，通过分析和光谱数据合成并评估了一类新型的混合甾体杂环化合物，这些衍生物的有效性得到了证明。采用 MTT 法检测了合成的化合物 2a、2b、2c、3b、8、10a、10b、13、14、16a 和 19 对三种人癌细胞系（乳腺癌细胞 MCF-7、前列腺癌细胞 PC3 和肝癌细胞 HepG2）的细胞毒性。在 24 小时孵育后，化合物 10a、10b、2c 和 14 对 MCF7、PC3 和 HepG2 的生长表现出比参考药物阿霉素（Dox）更强的抑制作用。值得注意的是，在这方面，测试的化合物 10a、10b、2c 和 14 表现出最显著的效果。结果通过形态学研究得到了证实。
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