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作为前列腺癌和乳腺癌迁移抑制剂的海洋萜烯 sarcophine 的半合成类似物。

Semisynthetic analogues of the marine cembranoid sarcophine as prostate and breast cancer migration inhibitors.

机构信息

Department of Basic Pharmaceutical Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71201, USA.

出版信息

Bioorg Med Chem. 2011 Aug 15;19(16):4928-34. doi: 10.1016/j.bmc.2011.06.060. Epub 2011 Jun 28.

Abstract

Sarcophine (1) is a bioactive cembranoid diterpene isolated from the Red Sea soft coral Sarcophyton glaucum. Previous semisynthesis attempts resulted in decreased or complete loss of 1's anticancer activity. Sarcophine and analogues showed antimigratory activity against breast and prostate cancer cell lines. This encouraged further semisynthestic optimizations to improve its activity and establish a preliminary structure-activity relationship. Eight new and five known semisynthetic analogues were generated. These compounds were evaluated for their ability to inhibit growth, proliferation, and migration of the prostate and breast metastatic cancer cell lines PC-3 and MDA-MB-231, respectively. Most analogues exhibited enhanced antimigratory activity.

摘要

sarcophine(1) 是一种从红海软珊瑚 sarcophyton glaucum 中分离出来的生物活性cembranoid 二萜。以前的半合成尝试导致 1 的抗癌活性降低或完全丧失。 sarcophine 和类似物对乳腺癌和前列腺癌细胞系显示出抗迁移活性。这鼓励进一步的半合成优化以提高其活性并建立初步的结构-活性关系。生成了 8 个新的和 5 个已知的半合成类似物。评估这些化合物抑制前列腺和乳腺癌转移癌细胞系 pc-3 和 mda-mb-231 生长、增殖和迁移的能力。大多数类似物表现出增强的抗迁移活性。

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