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Updated: Jul 18, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Linker-modified triamine-linked acridine dimers: synthesis and cytotoxicity properties in vitro and in vivo
Shan-Shue Wang1, Yi-Jen Lee, Shih-Chung Hsu
1Department of Biochemical Engineering, Kao Yuan University, 1821 Chung-Shan Rd, Lu-Chu Hsiang, Kaohsiung, Taiwan, ROC. sswang@cc.kyu.edu.tw
Abstract:
The preparation and cytotoxicity properties of a series of N(epsilon)-substituted triamine-linked acridine dimers are described. Most acridine dimer derivatives reveal highly potent in vitro cytotoxicity properties and DNA binding activity. Several acridine dimers were selected to study their action in vivo. These acridine dimers have demonstrated a narrow safe margin, as has adriamycin, but higher maximum tolerate dose (MTD) in comparison with that of adriamycin in ICR mice. The acridine dimers also demonstrated various anit-COLO 205 solid tumor activities in vivo. Compound 1 has shown the most potent solid tumor inhibition.
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