52093-45-5Relevant academic research and scientific papers
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors
Yang, Lingling,Ma, Xiaobo,Yuan, Chen,He, Yanying,Li, Ling,Fang, Sha,Xia, Wei,He, Tao,Qian, Shan,Xu, Zhihong,Li, Guobo,Wang, Zhouyu
, p. 230 - 241 (2017/04/19)
Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and selective SIRT2 inhibitors is currently desirable, which may provide a new strategy for treatment of related diseases. Herein, a structure-based optimization approach led to new 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as SIRT2 inhibitors. SAR analyses with new synthesized derivatives revealed a number of new potent SIRT2 inhibitors, among which 28e is the most potent inhibitor with an IC50 value of 42?nM. The selectivity analyses found that 28e has a very good selectivity to SIRT2 over SIRT1 and SIRT3. In cellular assays, 28e showed a potent ability to inhibit human breast cancer cell line MCF-7 and increase the acetylation of α-tubulin in a dose-dependent manner. This study will aid further efforts to develop highly potent and selective SIRT2 inhibitors for the treatment of cancer and other related diseases.
Novel SIRT2 protein inhibitor and usage thereof in pharmacy
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Paragraph 0114; 0115, (2017/08/28)
The invention discloses a compound or salt, crystallographic form and solvate compounds of the compound acceptable in pharmacy, and the compound and the salt, crystallographic form, solvate compounds of the compound are shown as formula I, wherein X is selected from the formulas (please see the specifications for the formula); R1 is selected from aryl or ceteroary or substituted aryl or substituted ceteroary or from the formula (please see the specifications for the formula); R2 is selected from the formulas (please see the specifications for the formula); and R3 is selected from halogen or C1-C4 alkyl or C1-C4 alkoxy. The novel compound shown in formula I has the advantages that not only is good inhibitory activity achieved to SIRT2, but also the inhibiting effect is achieved to the tumor, and the novel compound has good pharmaceutical potentiality and provides a novel potential choice for the clinical medicament.
HUMAN PLASMA KALLIKREIN INHIBITORS
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Page/Page column 556; 558, (2015/11/02)
Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
An enantiopure galactose oxidase model: synthesis of chiral amino alcohols through oxidative kinetic resolution catalyzed by a chiral copper complex
Mannam, Sreedevi,Sekar, Govindasamy
experimental part, p. 497 - 502 (2009/07/18)
An enantiopure galactose oxidase (GO) enzyme model has been synthesized from readily available (R)-BINAM and Cu(OTf)2, and the enantiopure GO model has been effectively used in situ as an efficient chiral catalyst for the synthesis of chiral amino alcohols through oxidative kinetic resolution (OKR), where molecular oxygen is used as the sole oxidant. Under the proposed catalytic conditions, both ortho- and para-substituted amino alcohols were resolved with good to excellent enantiomeric excesses through oxidative kinetic resolution.
