2. Academic Validation
  3. Linker-modified triamine-linked acridine dimers: synthesis and cytotoxicity properties in vitro and in vivo

Linker-modified triamine-linked acridine dimers: synthesis and cytotoxicity properties in vitro and in vivo

  • Bioorg Med Chem. 2007 Jan 15;15(2):735-48. doi: 10.1016/j.bmc.2006.10.054.
Shan-Shue Wang 1,  Yi-Jen Lee,  Shih-Chung Hsu,  Hsueh-O Chang,  Wei-Kung Yin,  Lien-Shange Chang,  Shan-Yen Chou
Affiliations

Affiliation

  • 1 Department of Biochemical Engineering, Kao Yuan University, 1821 Chung-Shan Rd, Lu-Chu Hsiang, Kaohsiung, Taiwan, ROC. sswang@cc.kyu.edu.tw
PMID: 17107806 DOI: 10.1016/j.bmc.2006.10.054
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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