Efficient and easy synthesis of octathymidylate covalently linked to intercalating 9-aminoellipticine

Add time:08/25/2019    Source:sciencedirect.com

Reductive amination of 3′-apurinic octathymidylate with 9-aminoellipticine provides octathymidylate covalently linked to intercalating ellipticine through a 3,4-dihydroxypentamethylene linker. Studies of its binding properties to poly(rA) reveals the formation of two different complexes depending of the temperature (Tm 13°C and 38°C) with dT/rA stoichiometry respectively equal to 2/1 and 1/1. When compared to parent octathymidylate, stability of the latter duplex is enhanced by the interaction energy provided by the dye moiety.

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