Pyrrolo[3′,2′:6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity

Pyrrolo[3′,2':6,7]cyclohepta[1,2-b]pyridines were synthesized as photosensitizing agents using a versatile synthetic pathway. Photobiological studies revealed that the majority of the new compounds showed a potent cytotoxic effect upon photoactivation, especially when decorated with a 2-ethoxycabonyl group and a N-benzyl substituted moiety, with EC50 values at submicromolar level and 1O2 quantum yields ΦR-400 = 0.26 ± 0.03.99