Abstract

Piscidinol A (1), a major compound isolated from Aphanamixis polystachya, 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 6e and 6i 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 6e and 6i 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

Piscidinol A ( 1 ) 是从Aphanamixis polystachya中分离出来的主要化合物，对癌细胞系表现出适度的抗癌活性。随后，通过修饰这种高产天然产物的关键结构功能合成了一系列类似物，并评估了它们对各种癌细胞系的抗癌潜力。在测试的衍生物中，化合物6e和6i分别在 5.38 和 5.02 µM 浓度下显着降低对 DU145 前列腺癌细胞的细胞活力。此外，这两种化合物均将细胞周期阻滞在 S 期，并诱导 DU145 细胞晚期凋亡。总之，结果表明化合物6e和6i可能是开发针对 DU145 的抗癌药物的有希望的先导，并且非常值得进一步研究，旨在产生潜在的抗癌药物。