Halogenated diarylacetylenes repress c-myc expression in cancer cells

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3638-40. doi: 10.1016/j.bmcl.2014.04.113. Epub 2014 May 9.

Abstract

Halogenated diarylacetylenes that possess fluorine or chlorine substituents in one aryl ring and N-methylamino or N,N-dimethylamino in the other aryl ring inhibit the proliferation of LS174T colon cancer cells through the repression of c-myc expression and induction of the cyclin-dependent kinase inhibitor-1 (i.e., p21(Wif1/Cip1)) and represent potentially useful antineoplastic agents.

Keywords: Antineoplastic agents; Colon cancer; Diarylacetylenes; c-myc.

Publication types

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

MeSH terms

  • Alkynes / chemistry*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Halogenation
  • Humans
  • Hydrocarbons, Chlorinated / chemical synthesis
  • Hydrocarbons, Chlorinated / chemistry
  • Hydrocarbons, Chlorinated / pharmacology*
  • Hydrocarbons, Fluorinated / chemical synthesis
  • Hydrocarbons, Fluorinated / chemistry
  • Hydrocarbons, Fluorinated / pharmacology*
  • Models, Molecular
  • Molecular Structure
  • Proto-Oncogene Proteins c-myc / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-myc / biosynthesis
  • Structure-Activity Relationship

Substances

  • Alkynes
  • Antineoplastic Agents
  • Hydrocarbons, Chlorinated
  • Hydrocarbons, Fluorinated
  • Proto-Oncogene Proteins c-myc