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.

中文翻译：

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泰洛佛林衍生物作为可能的抗肿瘤剂的设计、合成和体外评价

天然产物的结构简化和修饰一直是抗肿瘤药物的重要资源。通过在tylophorine的菲环中引入各种氨基甲基和酰胺基团，设计并合成了一系列新的tylophorine衍生物，并评估了它们对MCF-7、A549和HepG-2细胞的抗增殖活性。结果表明，大多数制备的化合物表现出良好的抗肿瘤活性。特别是，一种在侧链具有{乙基[2-(吗啉-4-基)乙基]氨基}甲基的化合物表现出最显着的细胞毒性作用。