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Synthesis, Cytotoxic and Heparanase Inhibition Studies of 5-oxo-1-arylpyrrolidine-3- carboxamides of Hydrazides and 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol

[ Vol. 17 , Issue. 3 ]

Author(s):

Swetha Hari, Toreshettahally R. Swaroop, Habbanakuppe D. Preetham, Chakrabhavi D. Mohan, Umashakara Muddegowda, Salundi Basappa, Israel Vlodavsky, Gautam Sethi and Kanchugarakoppal S. Rangappa*   Pages 243 - 250 ( 8 )

Abstract:


Design of chemically novel, biologically potent small heterocyclic molecules with anticancer activities, which targets the enzyme heparanase has gained prominent clinical interest. We have synthesized a novel class of carboxamide derivatives by coupling various substituted aromatic acid hydrazides and triazoleamine with pyrrolidine carboxylic acid by using coupling agents. The synthesized compounds are characterized by spectroscopic techniques such as FT-IR, HRMS and NMR. These compounds are investigated for cytotoxicity on different cancer cell lines and heparanase inhibitory activity. Most of them showed moderate heparanase inhibitory activity and good cytotoxicity.

Keywords:

Hydrazides, triazole, carboxamides, cytotoxicity, heparanase, pyrrolidine.

Affiliation:

Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, Department of Studies in Organic Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, Department of Studies in Molecular Biology, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, Department of Studies in Chemistry, Karnataka State Open University, Mukthagangothri, Mysuru-570006, Karnataka, Department of Studies in Organic Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka, Cancer and Vascular Biology Research Center, the Bruce, Rappaport Faculty of Medicine, Technion, Haifa, Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 117600, Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysuru-570006, Karnataka

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