作为前列腺癌的抗肿瘤药物的庚烯醇吡喃酮和吗啉酮。
Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer.
机构信息
Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA 30602-2352, USA.
出版信息
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.
摘要
合成了偕-烯醇吡喃-2-酮和吗啉-2-酮，并将其作为两种不同的前列腺人癌细胞系（PC-3 和 LNCaP）中细胞生长的抑制剂进行了评估。从 L-和 D-苯甘氨酸衍生出的类似物被发现是 LNCaP 和 PC-3 细胞生长的最有效拮抗剂。进一步的研究表明，这些抑制剂诱导 G2/M 期阻滞，并且基于苯甘氨酸的衍生物的（S）对映体是细胞溶质 iPLA(2)β 的更有效的抑制剂。
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