State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, P. R. China.
School of Basic Medicine, Guizhou University of Traditional Chinese Medicine, Dongqing South Road, Guizhou, 550025, P. R. China.
Chem Biodivers. 2020 Sep;17(9):e2000066. doi: 10.1002/cbdv.202000066. Epub 2020 Aug 3.
Structural simplification and modification of natural products are always very important resources to antitumor drugs. By introducing various aminomethyl groups and amide groups into the phenanthrene ring of tylophorine, a novel series of tylophorine derivatives have been designed and synthesized, and their antiproliferative activities against MCF-7, A549 and HepG-2 cells have been evaluated, too. The results indicated that most of the prepared compounds exhibited good antitumor activities. Especially, one compound with an {ethyl[2-(morpholin-4-yl)ethyl]amino}methyl group at the side chain exhibited the most significant cytotoxic effects.
结构简化和修饰天然产物一直是抗肿瘤药物的非常重要的资源。通过在千里光菲灵的菲环上引入各种氨甲基和酰胺基，设计并合成了一系列新型千里光菲灵衍生物，并对其对 MCF-7、A549 和 HepG-2 细胞的增殖活性进行了评价。结果表明，大多数所制备的化合物表现出良好的抗肿瘤活性。特别是，具有侧链上的{乙基[2-(吗啉-4-基)乙基]氨基}甲基的一个化合物表现出最显著的细胞毒性作用。
