ArticleMolecules (Basel, Switzerland)2015
An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-α Inducing Activity.
Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Interferon-α and its effects on cancer cell apoptosis.Oncology letters · 2022Review
- Tilorone: a Broad-Spectrum Antiviral Invented in the USA and Commercialized in Russia and beyond.Pharmaceutical research · 2020Article
- Modalities and Mechanisms of Treatment for Coronavirus Disease 2019.Frontiers in pharmacology · 2020Review
- Repurposing the antimalarial pyronaridine tetraphosphate to protect against Ebola virus infection.PLoS neglected tropical diseases · 2019Article
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tilorone dihydrochloride (1) has great potential for inducing interferon against pathogenic infection. In this paper, we describe a convenient preparation method for 2,7-dihydroxyfluoren-9-one (2), which is a usual pharmaceutical intermediate for preparing tilorone dihydrochloride (1). In the novel method, methyl esterification of 4,4'-dihydroxy-[1,1'-biphenyl]-2-carboxylic acid (4) was carried out under milder conditions with higher yield and played an important role in the preparation of compound 2. The structures of the relative intermediates and target compound were characterized by melting point, IR, MS, and ¹H-NMR. Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-α (IFN-α) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects.
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