Synthesis and biological evaluation of novel indenopyrazole derivatives

J Biochem Mol Toxicol. 2019 May;33(5):e22285. doi: 10.1002/jbt.22285. Epub 2019 Jan 23.

Abstract

A series of novel indenopyrazole derivatives 2a-j and 3a-j were synthesized from the reaction of 1-(4-(hydroxy(1-oxo-1,3-dihydro-2 H-inden-2-ylidene)methyl)phenyl)-3-phenylurea derivatives 1a-j with hydrazine and phenylhydrazine, respectively. The obtained novel indenopyrazoles ( 2a-j and 3a-j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay; 2a, 2b, 2d, 2h, and 3h were found to be the most active compounds. The compounds were also screened for antimicrobial activity, and all compounds showed moderate activity against used microorganisms.

Keywords: 2-Benzoylindan-1-one; anticancer; antimicrobial; apoptosis; ındenopyrazole.

MeSH terms

  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Proliferation / drug effects*
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Humans
  • Pyrazoles* / chemical synthesis
  • Pyrazoles* / chemistry
  • Pyrazoles* / pharmacology

Substances

  • Antineoplastic Agents
  • Pyrazoles