- Compound used as RET kinase inhibitor and application thereof
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The invention relates to a compound used as an RET kinase inhibitor and application thereof, wherein the compound has a structure as shown in a formula F, has good inhibition capability on RET kinase, and has good pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.
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Paragraph 0294-0298
(2021/07/01)
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- Structure-based modification of 3-/4-aminoacetophenones giving a profound change of activity on tyrosinase: From potent activators to highly efficient inhibitors
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In this study, we developed 3-/4-aminoacetophenones and their structure-based 3-/4-aminophenylethylidenethiosemicarbazide derivatives, respectively, as novel tyrosinase activators and inhibitors. Notably, all the obtained thiosemicarbazones displayed more potent tyrosinase inhibitory activities than kojic acid. Especially, compound 7k was found to be the most active tyrosinase inhibitor with IC50 value of 0.291 1/4M. The structure-activity relationships (SARs) analysis showed that: (1) the amine group was absolutely necessarily for determining the tyrosinase activation activity; (2) the introduction of thiosemicarbazide group played a very vital role in transforming tyrosinase activators into tyrosinase inhibitors; (3) the phenylethylenethiosemicarbazide moiety was crucial for determining the tyrosinase inhibitory activity; (4) the type of acyl group had no obvious effect on the inhibitory activity; (5) the position of amide substituent on the phenyl ring influenced the tyrosinase inhibitory potency. Moreover, the inhibition mechanism and inhibition kinetics study revealed that compound 7k was reversible and non-competitive inhibitor, and compound 8h was reversible and competitive-uncompetitive mixed-II type inhibitor.
- You, Ao,Zhou, Jie,Song, Senchuan,Zhu, Guoxun,Song, Huacan,Yi, Wei
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p. 255 - 262
(2015/03/04)
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- Synthesis of 3-trifluoroacetamidobenzoyltrifluoroacetone and its luminescent europium complexes
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Reaction of 3-aminoacetophenone with excess of methyl trifluoroacetate proceeds in two stages and leads to the formation of 3- trifluoroacetamidobenzoyltrifluoroacetone 3-CF3C(O)NHC 6H4C(O)CH2C(O)CF3
- Semenov,Zolotareva,Cherkasov
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body text
p. 874 - 879
(2012/09/22)
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- Photolabile compound and substrate for oligomer probe array with the same
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Provided is a substrate for an oligomer probe array to which a photolabile material having an acetylene derivative is directly attached or attached via a linker.
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Page/Page column 12
(2009/08/14)
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- Photolabile compound, oligomer probe array and substrate for oligomer probe array containing the same, and manufacturing method of the same
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A photolabile compound, an oligomer probe array, and a susbtrate for oligomer probe array comprising the same, and a manufacturing method of the same are disclosed. wherein, X is or R1 is hydrogen, an alkyl group, or an acetyl group, R2 is hydrogen, methyl, ethyl, propyl, or phenyl.
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Page/Page column 29
(2008/12/07)
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- N-(3-(IMIDAZO [1,5-A]PYRIMIDIN-4-YL)PHENYL]-SULFONAMIDES AND N-[3-(IMIDAZO[1,5-A]PYRIMIDIN-4-YL)-PHENYL]-CARBOXAMIDES AND THEIR USE AS GABAA RECEPTOR MODULATORS
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The present invention relates to compounds of formula I wherein R1, R2, R3 and X are as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by the 1 and 2-GABAA receptors.
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Page/Page column 7
(2008/06/13)
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- Mild deprotection of primary N-(p-toluenesulfonyl) amides with SmI 2 following trifluoroacetylation
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A mild deprotection method for notoriously difficult to unmask primary N-(p-toluenesulfonyl) amides was developed during our total synthesis studies toward the marine toxin, gymnodimine. The deprotection occurs at low temperature (-78 °C) under mild conditions by initial activation of the nitrogen with a trifluoroacetyl group, followed by reductive cleavage of the p-toluenesulfonyl group with samarium diiodide. The substrate scope and functional group tolerance of this useful N-S cleavage process, which builds on related cleavage processes of other nitrogen-heteroatom bonds, is explored. Georg Thieme Verlag Stuttgart.
- Moussa, Ziad,Romo, Daniel
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p. 3294 - 3298
(2008/09/17)
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- N-[3-(3-SUBSTITUTED-PYRAZOLO[1,5-a]PYRIMIDIN-7-YL)PHENYL]-SULFONAMIDES, AND COMPOSITIONS, AND METHODS RELATED THERETO
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The present invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the claims. The compounds have specific affinity for the GABAA receptor and are therefore useful in the treatmen
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Page/Page column 47; 48
(2008/06/13)
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