101417-40-7Relevant academic research and scientific papers
Amide derivatives and their medical use
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, (2018/04/21)
The invention relates to novel amide derivatives shown in a structural formula I in the specification or a pharmaceutically acceptable salt thereof, a medicine composition which takes the compounds as active components, and an application of the derivatives or the pharmaceutically acceptable salt of the derivatives to preparation of analgesia medicines. In the structural formula I, R1 and R2 are a hydrogen atom and a C1-C3 alkyl; R3 is hydrogen atom, C1-C3 alkyl, phenyl or a hydroxyl-substituted alkyl.
Pyrazolopyridine compound and use thereof
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Paragraph 0555; 0557; 0558, (2018/11/03)
The present invention relates to a pyrazolopyridine compound and use thereof, and further relates to a pharmaceutical composition comprising the pyrazolopyridine compound. The pyrazolopyridine compound or the pharmaceutical composition can be used as a so
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase
Lingel, Andreas,Sendzik, Martin,Huang, Ying,Shultz, Michael D.,Cantwell, John,Dillon, Michael P.,Fu, Xingnian,Fuller, John,Gabriel, Tobias,Gu, Justin,Jiang, Xiangqing,Li, Ling,Liang, Fang,McKenna, Maureen,Qi, Wei,Rao, Weijun,Sheng, Xijun,Shu, Wei,Sutton, James,Taft, Benjamin,Wang, Long,Zeng, Jue,Zhang, Hailong,Zhang, Maya,Zhao, Kehao,Lindvall, Mika,Bussiere, Dirksen E.
, p. 415 - 427 (2017/04/26)
PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin compaction and repression of tumor suppressor genes. Inhibiting this activity by small molecules targeting EZH2 was shown to result in antitumor efficacy. Here, we describe the optimization of a chemical series representing a new class of PRC2 inhibitors which acts allosterically via the trimethyllysine pocket of the noncatalytic EED subunit. Deconstruction of a larger and complex screening hit to a simple fragment-sized molecule followed by structure-guided regrowth and careful property modulation were employed to yield compounds which achieve submicromolar inhibition in functional assays and cellular activity. The resulting molecules can serve as a simplified entry point for lead optimization and can be utilized to study this new mechanism of PRC2 inhibition and the associated biology in detail.
PYRIDAZINONE COMPOUNDS AS CALCILYTICS
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Page/Page column 108-109, (2010/11/27)
Various calcilytic compounds and pharmaceutical compositions containing these compounds are disclosed. Calcilytic compounds are compounds capable of inhibiting calcium receptor activity. Methods for preparing calcilytic compounds, oral bioavailability of calcilytic compounds, and their use as calcium receptor antagonists are also disclosed.
The Synthesis of Hallachrome Leucotriacetate (2,7,8-Triacetoxy-1-methoxy-3-methylanthracene)
Comber, Mark F.,Sargent, Melvyn V.
, p. 1481 - 1489 (2007/10/02)
The synthesis of 2,7,8,-triacetoxy-1-methoxy-3-methylanthracene (30), a derivative of hallachrome (7-hydroxy-8-methoxy-6-methylanthracene-1,2-quinone) (1), the red pigment of the marine worm Halla parthenopeia (Delle Chiaje), is described.The key step in
