Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer.
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.
Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA 30602-2352, USA.
Jason N
JN
Mock
John P
JP
Taliaferro
Xiao
X
Lu
Sravan Kumar
SK
Patel
Brian S
BS
Cummings
Timothy E
TE
Long
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D008297:Male; D015394:Molecular Structure; D009025:Morpholines / Q000737:chemistry* / Q000494:pharmacology; D011471:Prostatic Neoplasms / Q000473:pathology*; D011714:Pyrans / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D009025:Morpholines; D011714:Pyrans; C037574:morpholine