School of Medicine, Huaqiao University, Quanzhou 362021, PR China.
School of Medicine, Huaqiao University, Quanzhou 362021, PR China.
Steroids. 2021 Feb;166:108776. doi: 10.1016/j.steroids.2020.108776. Epub 2020 Dec 15.
4β-Hydroxywithanolide E, which can be obtained in large amounts from the Physalis genus, possessed anti-proliferative effects on a variety of human cancer cell lines. For discussing its anti-tumor structure-activity relationship, a series of 4β-hydroxywithanolide E derivatives (1-17) were synthesized and evaluated for their antitumor activity in vitro towards acute promyelocytic leukemia NB4 cell line by the Alarma blue assay. Cytotoxicity data revealed that the enone structure and C-4 hydroxyl substituents of ring A, together with the side chain (C-20-C-28) play an important effect on the cytotoxicity.
4β-羟基羽扇豆烷内酯 E 可以大量从酸浆属植物中获得，对多种人类癌细胞系具有抗增殖作用。为了探讨其抗肿瘤构效关系，合成了一系列 4β-羟基羽扇豆烷内酯 E 衍生物（1-17），并通过 Alarma blue 测定法评估了它们对急性早幼粒细胞白血病 NB4 细胞系的体外抗肿瘤活性。细胞毒性数据表明，A 环中的烯酮结构和 C-4 羟基取代基以及侧链（C-20-C-28）对细胞毒性有重要影响。
