Synthesis and antioxidant and antitumor activity of novel pyridine, chromene, thiophene and thiazole derivatives

Arch Pharm (Weinheim). 2012 May;345(5):378-85. doi: 10.1002/ardp.201100335. Epub 2011 Dec 20.

Abstract

2-Tosylacetonitrile (1) when reacted with α,β-unsaturated nitriles 2a-c or a mixture of formaldehyde and 3-amino-2-substituted-pent-2-endinitriles 6a,b yielded pyridine derivatives 3a-c and 9a,b, respectively, while when subjected to react with salicylaldehyde yielded chromene derivatives 4 and 5, subsequently. The behavior of thiocarbamoyl derivative 10 derived from 1 towards some α-halogenated compounds have been investigated as well as its behavior towards elemental sulfur and phenyl isothiocyanate. Newly synthesized compounds were screened for their antioxidant activity, erythrocytes haemolysis and bleomycin-independent DNA damage. Some of the tested compounds exhibited promising activities.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antioxidants / chemical synthesis*
  • Antioxidants / pharmacology
  • Benzopyrans / chemical synthesis*
  • Benzopyrans / pharmacology
  • DNA Damage
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Rats
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Benzopyrans
  • Pyridines
  • Thiazoles
  • Thiophenes