Solid-phase synthesis of new pyrrolobenzodiazepine–chalcone conjugates: DNA-binding affinity and anticancer activity

A new class of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine–chalcone conjugates have been prepared by employing a solid-phase synthetic protocol. In this strategy an intramolecular aza-Wittig reductive cyclization approach has been utilized. Interestingly, some of these molecules have shown enhanced DNA-binding affinity and promising anticancer activity on a large number of human cancer cell lines.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide