Synthesis of New Series of Bis-Benzothiazole Derivatives as DNA Minor Groove Binding Agents

Ming-Li Yang and Xiu-Jun Wang

Abstract

A series of novel bis-benzothiazole derivaties with head-to head orientation were synthesised, and their anti-proliferative activities on U937, HL60 and HeLa cells were investigated. Most of these new compounds showed significant in vitro anticancer activity when compared to 5-FU. Molecular modeling, fluorescence and viscosimetry study showed that these compounds could bind into the minor groove of DNA.