2. Academic Validation
  3. Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer

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.
Jason N Mock 1,  John P Taliaferro,  Xiao Lu,  Sravan Kumar Patel,  Brian S Cummings,  Timothy E Long
Affiliations

Affiliation

  • 1 Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA 30602-2352, USA.
PMID: 22677312 DOI: 10.1016/j.bmcl.2012.05.038
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.

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