Small molecules capable of stabilizing the G-quadruplex structure have been shown to halt the proliferation of cancer cells, making quadruplexes interesting potential targets for development of improved anticancer drugs. We wished to investigate hybrid structures of known phenanthroline-based ligands. We have developed a convenient and high-yielding synthesis of a series of 4,7-diamino substituted 1,10-phenanthroline-2,9-dicarboxamides and evaluated their interactions with various G-quadruplex structures using FRET melting and CD spectroscopy. We will present the outcome of these studies, which resulted in the identification of potent ligands with high selectivity over duplex DNA and high aqueous solubility.

Tetrasubstituted phenanthrolines as potent G-quadruplex stabilizers

243rd National Meeting (2012)

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