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Bioorg Med Chem. 2008 Apr 15;16(8):4390-400. doi: 10.1016/j.bmc.2008.02.063. Epub 2008 Feb 23.

DNA threading bis(9-aminoacridine-4-carboxamides): effects of piperidine sidechains on DNA binding, cytotoxicity and cell cycle arrest.

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1
School of Medical Sciences, University of New South Wales, Sydney, NSW 2052, Australia.

Abstract

We describe the synthesis of a series of DNA-threading bis(9-aminoacridine-4-carboxamides) comprising ethylpiperidino and N-methylpiperidin-4-yl sidechains, joined via neutral flexible alkyl chains, charged flexible polyamine chains and a semi-rigid charged piperazine linker. Their cytotoxicity towards human leukaemic cells gives IC(50) values ranging from 99 to 1100 nM, with the ethylpiperidino series generally being more cytotoxic than the N-methylpiperidin-4-yl series. Measurements with supercoiled DNA indicate that they bisintercalate.

PMID:
18329887
DOI:
10.1016/j.bmc.2008.02.063
[Indexed for MEDLINE]
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