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Hwaseong, South Korea

Ryu Y.B.,Korea Research Institute of Bioscience and Biotechnology | Park S.-J.,Korea Research Institute of Bioscience and Biotechnology | Kim Y.M.,Korea Research Institute of Bioscience and Biotechnology | Lee J.-Y.,Hanmi Pharmaceutical Co. | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

Quinone-methide triterpenes, celastrol (1), pristimerin (2), tingenone (3), and iguesterin (4) were isolated from Triterygium regelii and dihydrocelastrol (5) was synthesized by hydrogenation under palladium catalyst. Isolated quinone-methide triterpenes (1-4) and 5 were evaluated for SARS-CoV 3CLpro inhibitory activities and showed potent inhibitory activities with IC50 values of 10.3, 5.5, 9.9, and 2.6 μM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC50 = 21.7 μM). As a result, quinone-methide moiety in A-ring and more hydrophobic E-ring assist to exhibit potent activity. Also, all quinone-methide triterpenes 1-4 have proven to be competitive by the kinetic analysis. © 2010 Elsevier Ltd. All rights reserved. Source


Trademark
Hanmi Pharmaceutical Co. | Date: 2016-02-12

Orally delivered oncology drug.


Trademark
Hanmi Pharmaceutical Co. | Date: 2016-02-26

Orally delivered oncology drug.


Trademark
Hanmi Pharmaceutical Co. | Date: 2016-02-26

Orally delivered oncology drug.


The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.

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