163210-97-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors
Zhang, Qingwei,Lu, Bingliu,Li, Jianqi
, p. 3162 - 3166 (2017)
The synthesis and biological evaluation of a variety of 4-piperazinyl-containing Chidamide derivatives is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below micromolar range, and inhibited proliferation of sev
ROR [gamma]t inhibitor, preparation method and application thereof
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Paragraph 1342; 1347-1349, (2021/07/08)
The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Paragraph 0653; 0656-0658, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
Preparation method of Bcl-2 family protein inhibitor synthesis intermediate
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Paragraph 0046; 0047; 0049; 0052; 0053; 0055, (2019/09/05)
The invention provides a preparation method of a Bcl-2 family protein inhibitor synthesis intermediate. The preparation method comprises the following steps: (a) taking methyl p-nitrobenzoate as a rawmaterial, enabling the material to react with sodium sulfide under the action of chloride to obtain a compound (2); (b) enabling the compound (2) to react with a compound (3) under an alkaline condition to obtain a compound (4); (c) enabling the compound (4) to react with a compound (5) under an alkaline condition to obtain a compound (6); (d) enabling ester ammonolysis reaction of the compound (6) and ammonia under the action of sodium methoxide and ethylene glycol to obtain a compound (1).
Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrin αiIbβ3
Krysko, Andrei A.,Samoylenko, Georgiy V.,Polishchuk, Pavel G.,Fonari, Marina S.,Kravtsov, Victor Ch.,Andronati, Sergei A.,Kabanova, Tatyana A.,Lipkowski, Janusz,Khristova, Tetiana M.,Kuz'Min, Victor E.,Kabanov, Vladimir M.,Krysko, Olga L.,Varnek, Alexandre A.
, p. 4646 - 4661 (2013/07/26)
A series of novel RGD mimetics containing phthalimidine fragment was designed and synthesized. Their antiaggregative activity determined by Born's method was shown to be due to inhibition of fibrinogen binding to αIIbβ3. Molecular docking of RGD mimetics to αIIbβ3 receptor showed the key interactions in this complex, and also some correlations have been observed between values of biological activity and docking scores. The single crystal X-ray data were obtained for five mimetics.
Deprotection of N-BOC compounds
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Page/Page column 4-5, (2009/08/18)
Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
Deprotection of N-BOC compounds
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Page/Page column 7-8, (2009/07/10)
Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture
Conte, Immacolata,Giuliano, Claudio,Ercolani, Caterina,Narjes, Frank,Koch, Uwe,Rowley, Michael,Altamura, Sergio,Francesco, Raffaele De,Neddermann, Petra,Migliaccio, Giovanni,Stansfield, Ian
scheme or table, p. 1779 - 1783 (2009/12/03)
The RNA replication machinery of HCV is a multi-subunit membrane-associated complex. NS5A has emerged as an active component of HCV replicase, possibly involved in regulation of viral replication and resistance to the antiviral effect of interferon. We report here substituted piperazinyl-N-(aryl)benzamides as potent inhibitors of HCV replication exerted via modulation of the dimerization of NS5A.
Novel practical deprotection of N-Boc compounds using fluorinated alcohols
Choy, Jason,Jaime-Figueroa, Saul,Jiang, Laurence,Wagner, Paul
, p. 3840 - 3853 (2008/12/23)
The thermolytic deprotection of N-Boc compounds was accomplished using TFE (2,2,2-trifluoroethanol) or HFIP (hexafluoroisopropanol) as solvents. Even though the cleavage of the t-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodology was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. Copyright Taylor & Francis Group, LLC.
PROCESS FOR MAKING SUBSTITUTED PIPERAZINYL COMPOUNDS
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Page/Page column 11, (2008/06/13)
A process for making a compound of formula (I): wherein R1 is C1 to C7 alkyl. The compounds having the formula (I) may be intermediates in a process for making dipeptide compounds, for example dipeptide nitrile compounds.
