A Series of Newsubstituted 4-(quinolin-4-ylamino)benzohydrazide derivatives were designed, synthesized, characterized by respective spectral data and evaluated for anti cancer activity. Most of the synthesized compounds showed good anti-cancer activityagainst MDA-MB-231, HeLa, SMMC-7721 cell lines. Among the compounds 8m and 8k having 2,6-dihydroxy, 3,4,5-trimethoxy substituents on the aromatic ring attached at the stereogenic center have shown equal potency to that of cisplatin with IC50 values were found to be the potent antiproliferative agents against MDA-MB-231, HeLa, SMMC-7721cellline with an IC50 value with 0.72±0.04 μM, 1.39±0.02 μM, 2.02±0.28 μM and 0.78±0.08 μM, 1.31±0.02 μM, 2.62±0.12 μMrespectively. Standard drug cisplatin exhibited IC50 values of 0.54±0.05 and 0.95±0.02 and 1.32±0.22 againstMDA-MB-231, HeLa, SMMC-7721. Compounds 8a, 8b were showed lower cytotoxic property in normal celllines. Docking studies of all the molecules disclosed close hydrogen bond interactions with the binding site.