Basing on the market multi-target antitumor agent sorafenib, a series of sixteen 4-4-(2-methyl- aminoacyl-pyridyl)oxylphenyl aryl thiourea derivatives were designed and synthesized.  Their structures were identified by the spectra of ¹H NMR, MS and elemental analysis.  The evaluation of antitumor bioactivities in vitro was done by MTT method.  It was shown that the synthesized compounds had antitumor activities and compounds 1a, 1d, 1i and 1j showed better or equal antitumor activity on sorafenib.