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■ Synthesis and DNA Cleavage Activity of 4,2’:4’,4’’:2’’,4’’’-Quaterthiazoles

Hideaki Sasaki

*Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Nishi-ku, Kobe 651-2113, Japan

Abstract

A series of 4,2’:4’,4”:2”,4’’’-quaterthiazole derivatives (2) were readily synthesized via a novel five-steps reaction. The key reaction involved the condensation of 1,4-dibromobutane-2,3-dione with two equimolar amounts of 2- (Boc-protected aminoalkyl)-thiazole-4-carbothioamide. The obtained 2,2’’’-bis-(3,6-diazahexyl)- and 2,2’’’-bis(3,6,9-triazanonyl)-4,2’:4’,4”:2”,4’’’-quaterthiazole (2b and 2c) exhibited significant affinity for double-stranded DNA, such as calf thymus DNA, as well as marked DNA cleavage activity in the presence of Co(II) ions under physiological conditions. Furthermore, the formation of a Co(II)-complex with 2b and 2c was found to be necessary for the DNA cleavage activity.