Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives

Arch Pharm (Weinheim). 2011 Feb;344(2):84-90. doi: 10.1002/ardp.201000201. Epub 2010 Nov 25.

Abstract

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC(50) value of about 1 µM. Compound 4f showed potent antifungal activity against Candida albicans (IC(50) = 1.29 µM) and compound 4h showed potent anticancer activity (IC(50) = 0.07 µM).

MeSH terms

  • Amidohydrolases / antagonists & inhibitors
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Drug Screening Assays, Antitumor / methods
  • HT29 Cells
  • Humans
  • Hydroxamic Acids / chemistry
  • Microbial Sensitivity Tests / methods
  • Molecular Structure
  • Structure-Activity Relationship
  • Thiosemicarbazones / chemical synthesis*
  • Thiosemicarbazones / chemistry
  • Thiosemicarbazones / pharmacology*
  • para-Aminobenzoates*

Substances

  • Anti-Infective Agents
  • Antineoplastic Agents
  • Hydroxamic Acids
  • Thiosemicarbazones
  • para-Aminobenzoates
  • Amidohydrolases
  • peptide deformylase