Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4854-8. doi: 10.1016/j.bmcl.2012.05.038. Epub 2012 May 17.

Abstract

Haloenol pyran-2-ones and morpholin-2-ones were synthesized and evaluated as inhibitors of cell growth in two different prostate human cancer cell lines (PC-3 and LNCaP). Analogs derived from L- and D-phenylglycine were found to be the most effective antagonists of LNCaP and PC-3 cell growth. Additional studies reveal that the inhibitors induced G2/M arrest and the (S)-enantiomer of the phenylglycine-based derivatives was a more potent inhibitor of cytosolic iPLA(2)β.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Humans
  • Male
  • Molecular Structure
  • Morpholines / chemistry*
  • Morpholines / pharmacology
  • Prostatic Neoplasms / pathology*
  • Pyrans / chemistry*
  • Pyrans / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Morpholines
  • Pyrans
  • morpholine