[摘要]:We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivs., e.g. I (R = Ph, R1 = H, Me, Br, MeO; R = Me, R1 = H, F, Me, MeO). These compds. had novel chem. structures that were distinct from those of previously reported inhibitors. Biol. data suggested that these compds. inhibited transforming growth factor-b signaling by interacting with the ATP-binding pocket of the transforming growth factor-b type I receptor kinase domain. Here, we report on the synthesis and structure-activity relationships of the compds. in this series.