Search Results - "Tao, Hongrui"
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Discovery of Novel PRMT5 Inhibitors by Virtual Screening and Biological Evaluations
Published in Chemical & pharmaceutical bulletin (01-04-2019)“…As an important epigenetics related enzyme, protein arginine methyltransferase 5 (PRMT5) has been confirmed as an anticancer therapeutic target in recent…”
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Identification and Assessments of Novel and Potent Small-Molecule Inhibitors of EED–EZH2 Interaction of Polycomb Repressive Complex 2 by Computational Methods and Biological Evaluations
Published in Chemical & pharmaceutical bulletin (01-01-2020)“…Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2…”
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Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations
Published in Bioorganic & medicinal chemistry letters (15-05-2018)“…[Display omitted] As one of the most promising anticancer target in protein arginine methyltransferase (PRMT) family, PRMT5 has been drawing more and more…”
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Discovery of New α-Glucosidase Inhibitors: Structure-Based Virtual Screening and Biological Evaluation
Published in Frontiers in chemistry (08-03-2021)“…α-Glycosidase inhibitors could inhibit the digestion of carbohydrates into glucose and promote glucose conversion, which have been used for the treatment of…”
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Identification of 5-benzylidene-2-phenylthiazolones as potent PRMT5 inhibitors by virtual screening, structural optimization and biological evaluations
Published in Bioorganic chemistry (01-12-2018)“…[Display omitted] •A class of PRMT5 inhibitors with the IC50 values ranging from 0.77 to 23 μM were identified.•The structure-activity relationship (SAR) of…”
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Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation
Published in European journal of medicinal chemistry (15-02-2019)“…Protein arginine methyltransferases 5 (PRMT5) represents an attractive drug target in epigenetic field for the treatment of leukemia and lymphoma. Here, a…”
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Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity
Published in Journal of computer-aided molecular design (01-08-2019)“…Protein arginine methyltransferase 5 (PRMT5) is responsible for the mono-methylation and symmetric dimethylation of arginine, and its expression level and…”
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Identification and assessments of novel and potent small-molecule inhibitors of EED-EZH2 interaction of polycomb repressive complex 2 by computational methods and biological evaluations
Published in Chemical and Pharmaceutical Bulletin (2019)“…Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2…”
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Asperbutenolide A, an unusual aromatic butenolide dimer with diverse bioactivities from a marine-derived fungus Aspergillus terreus SCAU011
Published in Tetrahedron letters (06-08-2020)“…[Display omitted] •Two new aromatic butenolide derivatives were obtained from a mangrove sediment derived Aspergillus fungus.•Asperbutenolide A (2) was an…”
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Interaction assessments of the first S-adenosylmethionine competitive inhibitor and the essential interacting partner methylosome protein 50 with protein arginine methyltransferase 5 by combined computational methods
Published in Biochemical and biophysical research communications (01-01-2018)“…Protein arginine methyltransferase 5 (PRMT5) is the most promising anticancer target in PRMT family. In this study, based on the first S-adenosylmethionine…”
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