PMID: 12614895Mar 5, 2003Paper

Bis-4-aminoquinolines: novel triple-helix DNA intercalators and antagonists of immunostimulatory CpG-oligodeoxynucleotides

Bioorganic & Medicinal Chemistry
Lucjan StrekowskiDonald E Macfarlane


Six dimeric 2-(2-naphthyl)quinolin-4-amines with a linker between the amino groups and eight dimeric 2-(4-anilino)quinolin-4-amines linked between the anilino groups were synthesized and evaluated for their interaction with duplex/triplex DNA's and as antagonists of immunostimulatory oligodeoxynucleotides with a CpG-motif (CpG-ODN). The most powerful triple-helix DNA intercalator known to date, with high affinity toward T.A.T triplets and triplex/duplex selectivity, was found. The potent antagonism of immunostimulatory CpG-ODN by several bis-4-aminoquinolines is not related to their DNA interactions.


Jan 1, 1991·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·C Hélène
Aug 15, 1995·Proceedings of the National Academy of Sciences of the United States of America·K R FoxS Neidle
Sep 27, 1996·Journal of Medicinal Chemistry·L StrekowskiW D Wilson
Apr 24, 1999·FEBS Letters·M KepplerK R Fox

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