Wu, Jie published the artcileDesign, synthesis, and screening of novel ursolic acid derivatives as potential anti-cancer agents that target the HIF-1α pathway, Computed Properties of 620-20-2, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(6), 853-858, database is CAplus and MEDLINE.
The transcription factor hypoxia-inducible factor-1α (HIF-1α) plays an important role in tumor angiogenesis, growth, and metastasis and is recognized as an important potential therapeutic target for cancer. Here, we designed and synthesized three novel series of ursolic acid derivatives containing an aminoguanidine moiety and evaluated them as HIF-1α inhibitors and anticancer agents using human cancer cell lines. Most of the compounds exhibited significant inhibition of HIF-1α transcriptional activity, as measured using a Hep3B cell-based luciferase reporter assay. Among these compounds, I was the most potent inhibitor of HIF-1α expression under hypoxic conditions (IC50 4.0 μM) and did not display significant cytotoxicity against any cell lines tested. The mechanism of action of I was investigated, we found that I downregulated HIF-1α protein expression, possibly by suppressing its synthesis, reduced production of vascular endothelial growth factor, and inhibited the proliferation of cancer cells.
Bioorganic & Medicinal Chemistry Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C12H10FeO4, Computed Properties of 620-20-2.
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https://en.wikipedia.org/wiki/Chloride,
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