Bioorganic & Medicinal Chemistry Letters 1998-01-20

Synthesis, DNA-damaging and cytotoxic properties of novel topoisomerase II-directed bisantrene analogues.

G Zagotto, A Oliva, F Guano, E Menta, G Capranico, M Palumbo

Index: Bioorg. Med. Chem. Lett. 8(2) , 121-6, (1998)

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Abstract

New bisantrene analogues were synthesized, bearing one or two 4,5-dihydro-1H-imidazol-2-yl hydrazone side chains at positions 1,4 or 9 of the anthracene ring system. A 10-azabioisostere was also prepared. The position of substituents in structurally isomeric drugs modulates topoisomerase II poisoning and specificity, along with cytotoxicity.