Synthesis and Preliminary Antitumor Activity of Distamycin Nitrogen Mustards

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

Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 1 , 2007

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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.

Keywords: Distamycin, Nitrogen mustard, DNA alkylation

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Article Details

Year: 2007
Page: [37 - 39]
Pages: 3
DOI: 10.2174/157018007778992955

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