56850-91-0Relevant academic research and scientific papers
Double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as preparation method and application thereof, pharmaceutical composition and medicament
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Paragraph 0429-0431, (2021/06/09)
The invention discloses a double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as a preparation method and application thereof, a pharmaceutical composition and a medicament, and belongs to the
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A2AReceptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents
Yan, Wenzhong,Ling, Lijun,Wu, Yiran,Yang, Kexin,Liu, Ruiquan,Zhang, Jinfeng,Zhao, Simeng,Zhong, Guisheng,Zhao, Suwen,Jiang, Hualiang,Xie, Chengying,Cheng, Jianjun
, p. 16573 - 16597 (2021/12/02)
Adenosine is an immunosuppressive factor in the tumor microenvironment mainly through activation of the A2A adenosine receptor (A2AR), which is a mechanism hijacked by tumors to escape immune surveillance. Small-molecule A2AR antagonists are being evaluat
Pyrene-containing water-soluble dye and preparation method thereof
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Paragraph 0058-0060, (2020/12/30)
The invention discloses a pyrene-containing water-soluble dye. The general formula of the pyrene-containing water-soluble dye is shown as a formula I. The pyrene-containing water-soluble dye with thewidened fluorescence emission spectrum is reasonable in
INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
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Page/Page column 78, (2019/08/26)
The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
New rosiglitazone analogue, preparation method and applications thereof
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Paragraph 0098-0102, (2020/01/12)
The invention relates to a rosiglitazone analogue, a preparation method and applications thereof, wherein the compound has a structure represented by the following formula (I), R1 represents C3-10 cycloalkyl unsubstituted or optionally substituted by the
Naphthylamine compound and biologically acceptable salt thereof as well as preparation method and application thereof
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Paragraph 0088; 0106; 0119-0121, (2019/12/15)
Aiming at shortage of anti-cancer targeting medicines in the prior art, the invention provides a naphthylamine compound and a biologically acceptable salt thereof as well as a preparation method and application thereof. By adopting the naphthylamine compo
PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Page/Page column 174, (2020/01/11)
Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
Discovery of Novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole Derivatives as Potential Anti-Inflammatory Agents
Li, Qing,Hu, Qinghua,Wang, Xinning,Zong, Yang,Zhao, Leilei,Xing, Junhao,Zhou, Jinpei,Zhang, Huibin
, p. 509 - 516 (2015/03/30)
A novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 5 with good anti-inflammatory activity was identified from our in-house library. Based on hit compound 5, two series of 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 6a-g and 7a-h were designed and synthesized as novel anti-inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF-α production in LPS-stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm) and TNF-α (IC50 = 1.87 μm) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti-inflammatory activity than ibuprofen did on xylene-induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF-κB in LPS-stimulated RAW 264.7 macrophages.
Development of unsymmetrical dyads as potent noncarbohydrate-based inhibitors against human β-N-acetyl-D-hexosaminidase
Guo, Peng,Chen, Qi,Liu, Tian,Xu, Lin,Yang, Qing,Qian, Xuhong
, p. 527 - 531 (2013/07/26)
Human β-N-acetyl-D-hexosaminidase has gained much attention due to its roles in several pathological processes and been considered as potential targets for disease therapy. A novel and efficient skeleton, which was an unsymmetrical dyad containing naphthalimide and methoxyphenyl moieties with an alkylamine spacer linkage as a noncarbohydrate-based inhibitor, was synthesized, and the activities were valuated against human β-N-acetyl-D- hexosaminidase. The most potent inhibitor exhibits high inhibitory activity with Ki values of 0.63 μM. The straightforward synthetic manners of these unsymmetrical dyads and understanding of the binding model could be advantageous for further structure optimization and development of new therapeutic agents for Hex-related diseases.
METHODS OF USING SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
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Page/Page column 98; 99, (2011/11/30)
Methods of using semi-synthetic glycopeptides of formula I-XIV having antibacterial activity are described.
