The Usefulness of Cyclic Diamidines with Different Core-substituents as Antitumor Agents

Jaroslaw Spychala

doi:https://doi.org/10.1016/j.bioorg.2008.05.002

The Usefulness of Cyclic Diamidines with Different Core-substituents as Antitumor Agents

Abstract

A series of related polycationic compds. has been screened for potential antitumor activity by the NCI's in vitro testing (one dose primary anticancer assay and the NCI-60 full panel screening). The GI50 values of triazines 3 and 4 are on av. 1.9 μM and 2.4 μM, resp. Furan 8 deserves mention too (1.9 μM). The biol. test results showed that carbazole 10 possessed cytotoxic activity in the nanomolar range, much better than the other compds. tested, only against several cancer cell lines: CCRF-CEM, HL-60(TB), MOLT-4, NCI-H522, COLO 205, SF-268, but the av. GI50 value was higher (15 μM). The activity appears closely dependent on the core-shape and length of the bisimidazoline mols. (important for both high cytotoxicity and DNA binding). The mechanism of DNA minor-groove binding of diamidines 1-12, based on the anticancer parameters, is highly probable.

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Jaroslaw Spychala dr

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Category:: Magazine publication
Type:: Magazine publication
Published in:: BIOORGANIC CHEMISTRY no. 36, edition 4, pages 183 - 189,
ISSN: 0045-2068
Publication year:: 2008
Bibliographic description:: Jaroslaw Spychala, The Usefulness of Cyclic Diamidines with Different Core-substituents as Antitumor Agents, Bioorganic Chemistry, vol. 36(4), pages 183-189, 2008.
DOI:: Digital Object Identifier (open in new tab) https://doi.org/10.1016/j.bioorg.2008.05.002
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