Design and synthesis of pyrrolo[2,1-][1,4]benzodiazepine (pbd)-polyaminoalkyl conjugates by the use of S_NAr beaction of 2-nitro-5-fluorobenzoate precursor as key reaction

摘要

The design and synthesis of a series of pyrrolo[2,1-c][1.4]benzodiazepine (PBD)-polyaminoalkyl conjugates as DNA minor groove binders are described.to introduced polyminoalkyl groups to the pyrrolo[2,1-c][1,4]benzodiazepine pharmacophore,S_NAr reactions between 2-nitro-5-fluorophenyl ketone or 2-nitro-3-pehenyl ketone adn polyaminoalkyl side chains were developed.