Thirteen 1,2-disubstituted hydrazines, including ten 2-aryl-1-(4-(N-isopropyl) aminoformyl)benzyl hydrazines (9a~9j), two 2-aryl methylene-1-(4-(N-isopropyl)aminoformyl)benzyl hydrazines (13a~13b), and 2-(4-methyl)benzoyl- 1-(4-(N-isopropyl)aminoformyl)benzyl hydrazine (14) have been designed and synthesized. By employing methyl thiazolyl tetrazolium (MTT) assay, generally all the title compounds were shown with better anti-cancer activity against rat glioma cells against the five cancer cell lines except both C6 and SW620 cell lines among the 13 title compounds, its IC₅₀ value against MDA-MB-231 cells was (10.8±0.9) μmol/L, whilst 13b was the most active against C6 cells with IC₅₀ value of (15.9±3.1) μmol/L, and 9e was the most active against SW620 cells with IC₅₀ value of (62.7±1.4) μmol/L. It was found that when the substituent in aryl group of 9a~9j was electron-withdrawal, the anti-cancer activity of compound with substituent at meta-position was better that at para-position (9g>9f, 9i>9h). Intriguingly, when the substituent was an electron-donor group, this law was lost. It was also identified that the anti-cancer activity against SW620 cells will be enhanced with the existence of a weak electron-donor inductive group. Mouse embryonic fibroblasts (3T3) were applied here. Compounds 9a, 9b, 13a, and 13b were displayed sensitive to this cell line. IC₅₀ values of 9a, and 13a were (24.9±1.2), and (13.9±1.7) μmol/L, respectively.