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新型鱼精蛋白 A 衍生物的合成及抗增殖活性研究——潜在的抗癌药物。

Synthesis and antiproliferative activities of novel piscidinol a derivatives as potential anticancer agents.

机构信息

Centre for Natural Products & Traditional Knowledge, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana, India.

Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana, India.

出版信息

Nat Prod Res. 2023 Jul-Aug;37(15):2568-2574. doi: 10.1080/14786419.2022.2056889. Epub 2022 Mar 27.

Abstract

Piscidinol A (), a major compound isolated from , showed modest anticancer activity against cancer cell lines. Subsequently, a series of analogues were synthesised by modification of the key structural functionalities of this high yield natural product and assessed for their anticancer potential against various cancer cell lines. Among the tested derivatives, the compounds and are significantly reduced the cell viability at 5.38 and 5.02 µM against DU145 prostate cancer cells, respectively. Additionally, both the compounds arrested the cell cycle at S phase and induced the late apoptosis in DU145 cells. Together, the results demonstrated that the compounds and could be a promising lead for the development of anticancer agents against DU145 and well worth further investigation aiming to generate potential anticancer agents.

摘要

鱼精蛋白 A(),从分离得到的主要化合物,对癌细胞系表现出适度的抗癌活性。随后,通过修饰该高产天然产物的关键结构官能团,合成了一系列类似物,并评估它们对各种癌细胞系的抗癌潜力。在所测试的衍生物中,化合物和分别以 5.38 和 5.02 μM 的浓度显著降低了前列腺癌细胞 DU145 的细胞活力。此外,这两种化合物都使 DU145 细胞的细胞周期停滞在 S 期,并诱导晚期细胞凋亡。总之,这些结果表明化合物和可能是开发针对 DU145 的抗癌药物的有前途的先导化合物,值得进一步研究以产生潜在的抗癌药物。

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