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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. © 2020 Wiley-VHCA AG, Zurich, Switzerland.


Zhiguo Mang, Shuai Zhang, Jing Bai, Meijuan Li, Hao Li. Design, Synthesis and in Vitro Evaluation of Tylophorine Derivatives as Possible Antitumor Agents. Chemistry & biodiversity. 2020 Sep;17(9):e2000066

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PMID: 32567792

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