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Updated: May 9, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, synthesis, and antitumor activity of novel podophyllotoxin derivatives as potent anticancer agents
1a General Unit of Chinese People's Armed Police Force Hospital , Jiangxi Nanchang 330001 , China.
Abstract:
In order to find novel synthetic compounds with superior antitumor activity and overcome multidrug resistance, a series of novel 4β-N-substituted podophyllotoxin derivatives were synthesized under mild conditions with satisfactory yield. Nine novel podophyllotoxin derivatives were synthesized by linking 4β-amino-podophyllotoxin with aldehydes via the formation of a Schiff's base, and imines were reducted to secondary amines. These novel derivatives have been evaluated for cytotoxicity against human cancer cell lines Hela, K562, and K562/AO2. The results indicated that these compounds possess superior bioactivity (IC50 values were found at the range of 10(- 6)-10(- 8) mol/l) and weak multidrug resistance.
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