A series of novel N-pyridyl-2-(4-aryloxyphenoxy) propionamide compounds were designed and prepared from the starting materials of (R)-2-(4-hydroxyphenoxy) propanoic acid and chloropyridine, and the structures were characterized by 1HNMR, 13CNMR, LC/MS, IR and elemental analysis．The effects of reaction conditions on the steric configuration were studied. Preliminary bioassay indicates that some compounds posed antitumor activity to A549 and Hela cells in vitro by MTT method. In particular, N-(3-nitropyridin-2-yl)-2-[4-[(6-chloroquinoxalin-2-yl) oxy]phenoxy] propanamide (Ⅳf) (IC50 = 0.007 mM) was more effective against A549 than drug cisplatin (IC50 = 0.026 mM).