Tetrasubstituted naphthalene diimide ligands with selectivity for telomeric G-quadruplexes and cancer cells.
作者： Sonja M. Hampel , Assitan Sidibe , Mekala Gunaratnam , Jean-François Riou , Stephen Neidle
DOI: 10.1016/J.BMCL.2010.09.066
关键词:
摘要: A series of tetrasubstituted naphthalene diimide compounds with N-methylpiperazine end groups has been synthesized and evaluated as G-quadruplex ligands. They have high affinity selectivity for telomeric DNA over duplex DNA. CD studies show that they induce formation a parallel topology. inhibit the binding hPOT1 topoisomerase IIIα to telomerase activity in MCF7 cells. The potent panel cancer cell lines, typical IC(50) values ∼0.1 μM, up 100-fold lower toxicity normal human fibroblast line.
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