Synthesis, DNA-binding ability and evaluation of antitumour activity of triazolo[1,2,4]benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates

A series of triazolobenzothiadiazine-pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepared. These compounds have exhibited significant cytotoxicity against most of the cell lines examined. Compound 5a displays GI50 values from 1.83 to 2.38 μM against seven human tumour cell lines, and is identified as a promising lead compound from this series. Their DNA thermal denaturation studies have also been carried out, and one of the compounds 5c elevates the DNA helix melting temperature of the CT-DNA by 2.6 °C after incubation for 36 h.

Novel triazolobenzothiadiazine–PBD conjugates were synthesized and exhibited significant anticancer activity against lung, breast, oral, colon, cervix, prostate and ovarian cancer cell lines.Figure optionsDownload as PowerPoint slide