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A novel azopyridine-based Ru(Ⅱ) complex [Ru(bpy)2(L1)2]2+ (bpy =2,2-bipyridine, L1 =4,4-azopyridine) was designed and synthesized as a potential glutathione (GSH)-responsive photoactivated chemotherapy (PACT) agent, the DNA covalent binding capability of which can be only activated after GSH reduction and visible light irradiation.