Natural Science Laboratory, Division of Medicinal and Pharmaceutical Chemistry, Department of Pharmaceutical Technology, Jadavpur University, Kolkata-700 032, India Indian Institute of Chemical Biology, 4, Raja S. C. Mullick Road, Jadavpur, Kolkata-700 032, India E-mail: tjupharm@yahoo.com Manuscript received online 03 July 2020, accepted 30 July 2020 Thirty 5-N-substituted-2-N-(arylsulphonyl)-L(+)glutamines were synthesized and evaluated biologically for their anticancer activities. The best active compound of this series showed 92.92% inhibition of tumor weight against Ehrlich Ascites Carcinoma cells. The most active compound was proved to be a competitive inhibitor of glutaminase in the enzyme assay. The best active compound may be a starting point to generate ‘lead’ for further exploration.