Synthesis and Preliminary Antitumor Activity of Distamycin Nitrogen Mustards

Title: Synthesis and Preliminary Antitumor Activity of Distamycin Nitrogen Mustards

Volume: 4 Issue: 1

Author(s): Yuqiang Wang, Zhaoqi Yang, Susan C. Wright and James W. Larrick

Affiliation:

Keywords: Distamycin, Nitrogen mustard, DNA alkylation

Abstract: Distamycin nitrogen mustard derivatives with different substituents at the amidino moiety located at the C-terminal of the peptide were synthesized. The in vitro antitumor activity was determined against human chronic leukemia K562 cells. Compound 3, bearing a terminal ethylamido group, had the best antitumor activity with an IC50 value of 0.72 μM. Compound 5, bearing a terminal dimethylamino group, had an IC50 value of 2.0 μM. This result suggests that a terminal positive charge is not essential for optimal antitumor activity.

Cite this article as:

Wang Yuqiang, Yang Zhaoqi, Wright C. Susan and Larrick W. James, Synthesis and Preliminary Antitumor Activity of Distamycin Nitrogen Mustards, Letters in Drug Design & Discovery 2007; 4 (1) . https://dx.doi.org/10.2174/157018007778992955