Synthesis and in vitro cytotoxicity evaluation of some fluorinated hexahydropyrimidine derivatives

Bioorg Med Chem Lett. 2011 Feb 1;21(3):989-92. doi: 10.1016/j.bmcl.2010.12.022. Epub 2010 Dec 10.

Abstract

A series of trifluoromethylated hexahydropyrimidine and tetrahydropyrimidine derivatives were synthesized and their in vitro cytotoxic activities were determined in colon cancer cell line (COLO 320 HSR). Compounds 4f, 4g, 4k, 5, and 7 proved to be the most active in this series of compounds. They represent promising new leads for the development of highly potent and selective anticancer compounds. All the compounds are lipophilic due to the trifluoromethyl group, and are thus expected to penetrate the membrane in appreciable concentration.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Halogenation
  • Humans
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Pyrimidines / toxicity
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyrimidines
  • pyrimidine