Synthesis, antioxidant, and cytotoxic activities of N-azole substituted thiomorpholine derivatives

Arch Pharm (Weinheim). 2014 Mar;347(3):221-8. doi: 10.1002/ardp.201300299. Epub 2014 Jan 7.

Abstract

A new class of N-azole substituted thiomorpholine derivatives were prepared and their antioxidant and cytotoxic activities were studied. The methyl substituted oxazolyl thiomorpholine dioxide 9b exhibited radical scavenging activity greater than the standard ascorbic acid. On the other hand, the thiazolyl thiomorpholine 10c having a chloro substituent on the aromatic ring was identified as a remarkable lead molecule for cytotoxic activity against A549 and HeLa cells, with IC50 values of 10.1 and 30.0 µM, respectively.

Keywords: Antioxidant activity; Cytotoxicity; Imidazoles; Oxazoles; Thiazoles; Thiomorpholines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Antioxidants / chemical synthesis*
  • Antioxidants / pharmacology*
  • Azoles / chemical synthesis*
  • Azoles / pharmacology*
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • HeLa Cells
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Morpholines / chemical synthesis*
  • Morpholines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Azoles
  • Morpholines
  • thiamorpholine