Synthesis and antitumor properties of an anthraquinone bisubstituted by the copper chelating peptide Gly-Gly-L-His

E Morier-Teissier, N Boitte, N Helbecque…

Index: Morier-Teissier; Boitte; Helbecque; Bernier; Pommery; Duvalet; Fournier; Hecquet; Catteau; Henichart Journal of Medicinal Chemistry, 1993 , vol. 36, # 15 p. 2084 - 2090

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Citation Number: 48

Abstract

A new molecule 4 [(GGH-DAE) 2DHQl associating the 1, 4, 5, 8-tetrahydroxyanthraquinone ring (DHQ) of the antitumor drug mitoxantrone (2), two diaminoethylene chains (DAE), and the metalchelating peptide Gly-Gly-His (GGH) has been synthesized. Such a molecule presents characteristics able to induce antitumor activity: compound 4 intercalates into DNA as measured by ATm, fluorescence quenching, and viscometry; ESR studies demonstrate ...