期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 12, 页码 1440-1445出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.04.028
关键词
Ursolic acid; Tetrazole; HIF-1 alpha inhibitor; Cytotoxicity
资金
- National Science Foundation of China [81660608]
- Natural Science Foundation of Jilin Province [20160101218JC]
- Edanz Group China
The hypoxia-inducible factor-la (HIF-1 alpha) pathway has been implicated in tumor angiogenesis, growth, and metastasis. Therefore, the inhibition of this pathway is an important therapeutic target for the treatment of various types of cancers. Here, we designed and synthesized 31 ursolic acid (UA) derivatives containing a tetrazole moiety and evaluated them for their potential anti-tumor activities as HIF-la transcriptional inhibitors. Of these, compound 14d (IC50 0.8 +/- 0.2 mu M) displayed the most potent activity and compounds 14a (IC50 4.7 +/- 0.2 mu M) exhibited the most promising biological profile. Analysis of the structure-activity relationships of these compounds with HIF-1 alpha suggested that the presence of a tetrazole group located at C-28 of the UA derivatives was critical for their inhibitory activities.
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