Oxazole-containing macrocycles represent a promising class of anticancer agents that target the G-quadruplex structural form. This presentation will emphasize the quadruplex-targeting, cytotoxicity, and in vivoantitumor properties of a series of synthetic oxazole-containing macrocyclic compounds. These properties include the following:Highly selective binding to the G-quadruplex form of both DNA and RNA, with little or no affinity for the duplex or triplex form of either nucleic acid.A nonintercalative, �terminal capping� mode of binding to G-quadruplex structures.Potent anti-proliferative activity versus both telomerase-positive and telomerase-negative human tumor cells, suggesting that the anti-proliferative activity of the compounds is independent of telomerase status.Induction of rapid apoptotic cell death and cell cycle arrest at the prometaphase stage of mitosis.In vivo antitumor efficacy in athymic nude mice containing human breast tumor xenografts.

Macrocyclic polyoxazoles as highly selective G-quadruplex ligands

247th National Meeting (2014)

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