新型4-(1-金刚烷基)苯基类似物作为HIF-1α抑制剂的设计、合成及构效关系研究
Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors.
作者信息
Xia Yan, Duan Qiong, Zhao Bao-Hua, Li Dong-Feng, Hou Rui-Bin
机构信息
Laboratory of Photoelectric Material, Advanced Institute of Materials Science, Changchun University of Technology, 130012, Changchun, P. R. China.
Department of Chemistry, College of Chemistry and Life Science, Changchun University of Technology, 130012, Changchun, P. R. China.
出版信息
Med Chem. 2016;12(4):338-46. doi: 10.2174/1573406412666151109113007.
Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt tumor hypoxic condition. In this study, a series of adamantane-based compounds were synthesized and evaluated as potential inhibitors of HIF-1α. Examination of their structure-activity relationship (SAR) identified the adamantane-containing indole derivative 20a as a potent inhibitor of HIF-1α in Hep3B cell lines under tumor hypoxia (IC50 = 0.02 µM). The study herein may provide valuable information for the development of novel therapeutics against cancer and tumor angiogenesis.
缺氧诱导因子-1（HIF-1）是癌细胞适应肿瘤缺氧状态的关键介质。在本研究中，合成了一系列基于金刚烷的化合物，并评估其作为HIF-1α潜在抑制剂的活性。对其构效关系（SAR）的研究确定含金刚烷的吲哚衍生物20a在肿瘤缺氧条件下的Hep3B细胞系中是一种有效的HIF-1α抑制剂（IC50 = 0.02 μM）。本文的研究可能为开发针对癌症和肿瘤血管生成的新型治疗药物提供有价值的信息。
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