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

Swetha Hari, Toreshettahally R. Swaroop, Habbanakuppe D. Preetham, Chakrabhavi D. Mohan, Umashakara Muddegowda, Salundi Basappa, Israel Vlodavsky, Gautam Sethi, Kanchugarakoppal S. Rangappa

Research output: Contribution to journalLetterpeer-review

5 Scopus citations

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.

Original languageEnglish
Pages (from-to)243-250
Number of pages8
JournalCurrent Organic Synthesis
Volume17
Issue number3
DOIs
StatePublished - 2020

Keywords

  • Hydrazides
  • carboxamides
  • cytotoxicity
  • heparanase
  • pyrrolidine
  • triazole.

ASJC Scopus subject areas

  • Biochemistry
  • Organic Chemistry

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