A series of new cinnamido-pyrrolo [2, 1-c][1, 4] benzodiazepine conjugates (4a–d and 5a–d) and their dimers (6a–d) have been designed, synthesized and evaluated for their biological activity. The anticancer screening of compound 4a by the NCI exhibited significant GI50 values ranging from 68 to 732 nM against 53 of 59 human cancer cell lines tested. Compounds 5a–d and 6a–d have also shown remarkable cytotoxic activity with GI50 ...