1002309-47-8Relevant articles and documents
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity
Yu, Wensheng,Liu, Jian,Clausen, Dane,Yu, Younong,Duffy, Joseph L.,Wang, Ming,Xu, Shouning,Deng, Lin,Suzuki, Takao,Chung, Christine C.,Myers, Robert W.,Klein, Daniel J.,Fells, James I.,Holloway, M. Katharine,Wu, Jin,Wu, Guoxin,Howell, Bonnie J.,Barnard, Richard J. O.,Kozlowski, Joseph
, p. 4709 - 4729 (2021)
We describe the discovery of histone deacetylase (HDACs) 1, 2, and 3 inhibitors with ethyl ketone as the zinc-binding group. These HDACs 1, 2, and 3 inhibitors have good enzymatic and cellular activity. Their serum shift in cellular potency has been minimized, and selectivity against hERG has been improved. They are also highly selective over HDACs 6 and 8. These inhibitors contain a variety of substituted heterocycles on the imidazole or oxazole scaffold. Compounds 31 and 48 stand out due to their good potency, high selectivity over HDACs 6 and 8, reduced hERG activity, optimized serum shift in cellular potency, and good rat and dog PK profiles.
CDK6/DYRK2 Double-target inhibitor as well as preparation method and application thereof
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Paragraph 0041-0042, (2021/02/24)
The present invention discloses a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. The invention also discloses a preparation method of the compound and application of the compound in prevention and/or treatment of cancers or tumor-related diseases, especially breast cancer, prostate cancer, lung cancer, multiple myeloma, leukemia, gastric cancer, ovarian cancer, colon cancer, liver cancer, pancreatic cancer, human glioma and other diseases. The compound provided by the invention is expected to be developed into a new generation of anti-cancer drugs.
FUSED RING DERIVATIVE AS A2A RECEPTOR INHIBITOR
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Paragraph 0145-0147, (2020/08/09)
Disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an application of the compound or slat in preparation of drugs for treating diseases related to an A2A receptor.