• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Archiv der Pharmazie >Pharmacological explorations of eco-friendly amide substituted (Z)-beta-enaminones as anti-breast cancer drugs
【24h】

Pharmacological explorations of eco-friendly amide substituted (Z)-beta-enaminones as anti-breast cancer drugs

机译：生态酰胺酰胺取代（Z）-β-烯酮作为抗乳腺癌药物的药理探索

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Amide substituted (Z)-beta-enaminones were synthesized by green chemistry and stereo-specific synthetic pathway as novel phosphoinositide 3-kinase (PI3K) inhibitors and breast cancer drugs. PI3K inhibition was measured by competitive ELISA. A panel of cancer cell lines including MCF-7 (breast cancer), G-361 (skin cancer), and HCT 116 (colon cancer) were used to assess the anticancer potentials. In the PI3K assay, 2c and 2f were indolent for the proposed inhibitory action, which was recognized from the obtained IC50 (1.0 mu M). Excellent activity potential of 2a, 2b, and 2d was recognized from the IC50 range (0.05 mu M) whereas an intermediate action potential was observed for compounds 2e and 2i (IC50 0.1 and 0.25, respectively). The docking results exclusively proposed that the hydrophobic interactions in the PI3K binding pocket were overwhelmed by the binding affinity of the most potent ligands (2a, 2b, and 2d: inhibitory constant K-i = 18.16, 84.87, and 56.14 nM). MTT assay results revealed the antiproliferative activity domination of selected compounds (2a, 2b, and 2d) toward MCF-7. The relative activities of 2a, 2b, and 2d of 84.56, 80.87, and 90.12%, respectively, were comparable to that of the standard, doxorubicin (82.16%). SAR studies demonstrated amide substituted (Z)-beta-enaminones as precise PI3K inhibitors to treat breast cancer.
机译：通过绿色化学和立体特异性合成途径合成酰胺取代的（Z）--β-烯胺，作为新型磷酸钠3-激酶（PI3K）抑制剂和乳腺癌药物。通过竞争力的ELISA测量PI3K抑制。使用包括MCF-7（乳腺癌），G-361（皮肤癌）和HCT 116（结肠癌）的癌细胞系，评估抗癌潜力。在PI3K测定中，2℃和2F对于所提出的抑制作用是惰性的，该抑制作用是从所得IC50（＆ 1.0 mu m）的识别。从IC50范围（<0.05μm）识别出优异的2A，2B和2D的活性电位，而分别观察到化合物2E和2I（IC 50 0.1和0.25）的中间作用电位。基于最有效配体的结合亲和力（2a，2b，2d：抑制常数K-i = 18.16,84.87和56.16,84.87和56.16,84.87和56.16,84.87和56.16,84.87和56.14nm），分别提出了Pi3k结合袋中的疏水相互作用被最有效配体（2a，2b和2d：抑制常数K-i = 18.16,84.87和56.14nm）所淹没。 MTT测定结果揭示了所选化合物（2a，2b和2d）的抗增殖活性偏向MCF-7。分别为84.56,80.87和90.12％的2a，2b和2d的相对活性与标准，多柔比星（82.16％）的相对活性。 SAR研究表明酰胺取代（Z）-β-烯酮作为精确的PI3K抑制剂治疗乳腺癌。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号