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Updated: Apr 29, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of novel podophyllotoxin analogs as antitumor agents
Zhong-Heng Zhang1, Li-Ming Zhang, Gang Luo
1a Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics , School of Pharmacy, Tianjin Medical University , Tianjin 300070 , China.
Abstract:
A series of 4β N-indole-substituted podophyllotoxin derivatives were synthesized. Nine target compounds were evaluated against human cancer cell lines (HeLa, K562, and K562/A02) using MTT assay including three imine derivatives 8, 9, and 10 in vitro. The result showed that the three compounds had higher antitumor activity than their reduced forms. Among them, compounds 8, 9, 11, and 16 were superior to the positive control VP-16.
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