Synthesis and Biological Evaluation of a Benz[crf]indol-2(1H)-one Derivatives

摘要

Virtual screening ot a library of 6.4 million compounds versus the structure of Xenopus Laevis' Aurora B kinase identified l-(n-propyl)-6-[2-(carboxyl)tetrahydropyrrol-l-yl]sulfonyl-benzo[cd]indol-2(1H)-one 1 as a possible lead compound. Then, a novel series of benz[cd]indol-2( 1 H)-one derivatives were synthesized and evaluated as Aurora B kinase inhibitors. The structures of the synthetic compounds were confirmed by 'H NMR, IR, mass spectrometry and elemental analysis. These compounds were evaluated by in vitro enzyme assay using spectrophotometry. Among them, compound 7e displayed potent antitumor activity against Aurora B kinase.