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Synthesis, biological evaluation, and enzyme assay of some 5-N-substituted-2-N-(arylsulphonyl)-L(+)glutamines as potential anticancer agents
Author : Tarun Jha *a, Soma Samanta a, Amit Kumar Halder a, Nilanjan Adhikari a, Sk. Abdul Amin a, Arpita Sanyal b and Tanmoy Mukherjee b
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ABSTRACT
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.
KEYWORD
Anticancer agent, glutamine derivative, glutaminase inhibition, inhibition assay