DNA threading agents: effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides

M Searcey, PN Martin, NM Howarth, B Madden…

文献索引：Searcey, Mark; Martin, P. Noel; Howarth, Nicola M.; Madden, Bernie; Wakelin, Laurence P. G. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 15 p. 1831 - 1836

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被引用次数: 7

摘要

A series of 9-anilinoacridine-4-carboxamides with cycloalkyl sidechains has been synthesised to study the effect of sidechain bulk on the DNA binding properties and biological activity of these potential threading intercalators. With sidechains larger than cyclohexane the pKa of the acridine is exceptionally low, so that DNA binding is restricted to pHs below 5. The compounds are cytotoxic to human colon carcinoma cells in the μM ...