Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents

A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities.  Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC₅₀ values of 2.52 and 1.99 μg·mL^–1, respectively.  Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection.  Our results provided a basis for the development of a new series of anti-cancer candidates.