In the present work few novel 2-(4-methylbenzenesulphonamido)pentanedioic acid bis amide derivatives and the basic compound 2-(4-methylphenylsulfonamido)pentanedioic acid have been synthesized, characterized and screened for their possible antineoplastic activity both in vitro and in vivo . The in vitro activity was performed against five human cell lines like human breast cancer (MCF-7), leukemia (K-562), ovarian cancer (OVACAR-3), human colon adenocarcinoma (HT-29) and Human kidney carcinoma (A-498). The in vivo activity was performed in female swiss albino mice against Ehrlich ascites carcinoma (EAC). Among the synthesized compounds, ureide, anilide, p -nitoanilide and o -bromoanilide derivatives of 2-(4-methyl benzene sulphonyl)-pentanedioic acid bis amides showed encouraging activity in both the in vitro and in vivo compared to other compounds. DOI: http://dx.doi.org/10.3329/bjp.v9i4.19774