5-Substituted [1]pyrindine derivatives with antiproliferative activity

Eur J Med Chem. 2010 Mar;45(3):896-901. doi: 10.1016/j.ejmech.2009.11.028. Epub 2009 Dec 6.

Abstract

We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but have interestingly no effect against the normal human fibroblasts CRL-2796. Generally, these pyrindines are active on both tumor cell lines. Compounds bearing large substituents with structural rigidity at position 5 such as phenyl-furyl show no inhibition of cell growth.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Fibroblasts / drug effects
  • HeLa Cells
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Pyridines / chemistry*

Substances

  • Antineoplastic Agents
  • Pyridines