Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer

…, JP Taliaferro, X Lu, SK Patel, BS Cummings…

Index: Mock, Jason N.; Taliaferro, John P.; Lu, Xiao; Patel, Sravan Kumar; Cummings, Brian S.; Long, Timothy E. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4854 - 4858

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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 ...