1,2,4-Benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: Synthesis, DNA-binding affinity and cytotoxicity

Benzothiadiazine–pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepared. These new classes of hybrid molecules exhibit cytotoxicity against many cancer cell lines. Their DNA thermal denaturation studies have been carried out and one of the compounds (4b) elevates the DNA helix melting temperature of the CT-DNA by 6.7 °C after incubation for 36 h.

Graphical abstractNovel 1,2,4-benzothiadiazine–PBD conjugates were synthesized and displayed significant anticancer activity against selected human cancer cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide