Wortmannilactones I–L, new NADH-fumarate reductase inhibitors, induced by adding suberoylanilide hydroxamic acid to the culture medium of Talaromyces wortmannii
| Autor: | Yi-Yu Wang, Jun-Hui Liu, Xinhua Lu, Yuesheng Dong, Zhihui Zheng, Wen-Cai Liu, Ke Aibing, Zhilong Xiu, Yu-Shi Luan |
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| Rok vydání: | 2016 |
| Předmět: |
Oxidoreductases Acting on CH-CH Group Donors
Stereochemistry Clinical Biochemistry Pharmaceutical Science Reductase Hydroxamic Acids 010402 general chemistry 01 natural sciences Biochemistry Talaromyces wortmannii Suberoylanilide Hydroxamic Acid Drug Discovery Ic50 values Molecular Biology NADH-fumarate reductase Vorinostat Molecular Structure 010405 organic chemistry Chemistry Spectrum Analysis Organic Chemistry Culture Media 0104 chemical sciences Talaromyces Molecular Medicine Macrolides |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:5328-5333 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2016.09.032 |
| Popis: | With the aim of finding more potential inhibitors against NADH-fumarate reductase (specific target for treating helminthiasis and cancer) from natural resources, Talaromyces wortmannii was treated with the epigenome regulatory agent suberoylanilide hydroxamic acid, which resulted in the isolation of four new wortmannilactones derivatives (wortmannilactones I-L, 1-4). The structures of these new compounds were elucidated based on IR, HRESIMS and NMR spectroscopic data analyses. These four new compounds showed potent inhibitory activity against NADH-fumarate reductase with the IC50 values ranging from 0.84 to 1.35μM. |
| Databáze: | OpenAIRE |
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