Synthesis of novel building blocks of 1H-pyrrolo[3,4-b]quinolin-3(2H)-one and evaluation of their antitumor activity

A series of new building blocks consisting of 1 H -pyrrolo[3,4- b ]quinolin-3(2 H )-one with potential as selective antitumor agents is described. Compounds were synthesized by using Heck reaction of N -allyl-1 H -pyrrolo[3,4- b ]quinolin-3(2 H )-one with p -bromophenyl acetic acid followed by formation of amide ( 1a–h , 2a–d ) by reaction with several secondary amines in good yields. The cytotoxicity of these compounds was evaluated against human cancer cell lines in vitro (SK–N–NH, A549). Studies suggest that most of these compounds were effective in inhibiting neuroblastoma cell growth, compound 1d was the most potent one (% IC 50 = 8.62 μM).