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Current Organic Synthesis


ISSN (Print): 1570-1794
ISSN (Online): 1875-6271

Letter Article

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

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*

Volume 17 , Issue 3 , 2020

Page: [243 - 250] Pages: 8

DOI: 10.2174/1570179417666200225123329

Price: $65


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.

Graphical Abstract
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