Abstract
The novel heterocyclophanes, 3, 6, 21, 24-tetraaza[8.8](2, 2')(4, 4'-bithiazolophane) (3a) and 3, 7, 22, 26-tetraaza-[9.9](2, 2')(4, 4'-bithiazolophane) (3b) were readily synthesized by the cyclization of 1, 4-dibromobutane-2, 3-dione with N, N'-bis(tert-butoxycarbonyl)ethylenediamine-N, N'-dipropionthioamide and N, N'-bis(tert-butoxycarbonyl)-trimethylenediamine-N, N'-dipropionthioamide, respectively, followed by acidic deprotection. Under physiological conditions, 3a and 3b at 5 μM showed considerable DNA-cleaving activities in the presence of Co(II) without any reducing agent.
