New anticancer active phenylene-bisbenzothiazoles: Synthesis, antiproliferative evaluation and DNA binding

Novel amidino substituted derivatives of phenylene-bis-benzothiazoles were synthesized and their antiproliferative activity against several human cancer cell lines, as well as DNA-binding features were determined. All tested compounds showed antiproliferative effects on tumour cells in a time- and concentration- dependent manner. The strongest activity was observed for b. These effects were shown to be related to DNA-binding properties, topoisomerase I and II poisoning effects and apoptosis induction. The highest tested selectivity towards tumor cells was observed for compound d that showed no cytotoxic effects on normal fibroblasts.