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Tetrahedron Lett. 2002 Aug 5;43(32):5621-5624. doi: 10.1016/S0040-4039(02)01113-9. Epub 2002 Jul 17.
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Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance.具有潜力和选择性的谷胱甘肽 S-转移酶 ω-1 抑制剂，可破坏癌症耐药性。
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Inhibition of calcium-independent phospholipase A2 activates p38 MAPK signaling pathways during cytostasis in prostate cancer cells.在前列腺癌细胞的细胞静止期间，抑制钙非依赖性磷脂酶 A2 会激活 p38 MAPK 信号通路。
Biochem Pharmacol. 2010 Jun 15;79(12):1727-35. doi: 10.1016/j.bcp.2010.02.005. Epub 2010 Feb 18.
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Role of Ca2+-independent phospholipase A2 in cell growth and signaling.钙离子非依赖性磷脂酶A2在细胞生长和信号传导中的作用。
Biochem Pharmacol. 2008 Oct 30;76(9):1059-67. doi: 10.1016/j.bcp.2008.07.044. Epub 2008 Aug 15.
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Inhibition of Ca2+-independent phospholipase A2 decreases prostate cancer cell growth by p53-dependent and independent mechanisms.非钙离子依赖型磷脂酶A2的抑制通过p53依赖和非依赖机制降低前列腺癌细胞的生长。
J Pharmacol Exp Ther. 2008 Jul;326(1):59-68. doi: 10.1124/jpet.108.138958. Epub 2008 Apr 25.
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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.

DOI:10.1016/j.bmcl.2012.05.038
PMID:22677312
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3376906/
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。