- Novel triazole derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating Aurora Kinase relating diseases containing the same as an active ingredient
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The present invention relates to a novel triazole derivative, a production method thereof, and an aurora kinase-associated pharmaceutical composition containing the same as an active ingredient. According to the present invention, the novel triazole derivative, an optical isomer thereof, or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activities as aurora kinase at nanomolar scale, thereby showing effectiveness in the treatment of various types of cancer or tumor as the pharmaceutical composition containing the same.COPYRIGHT KIPO 2017
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Paragraph 0177
(2017/08/02)
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- Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors
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A series of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives were designed, synthesized, and evaluated for the Aurora kinase inhibitory activities. The novel hinge-binder tethered 1,2,3-triazolylsalicylamide scaffold was effectively assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). A variety of alkynes with hinge binders were used to search proper structures-binding relationship to the hinge region. The synthesized 1,2,3-triazolylsalicylamide derivatives showed significant Aurora kinase inhibitory activity. In particular, 8a inhibited Aurora A kinase with an IC50 value of 0.284 μM, whereas 8m inhibited Aurora B kinase with an IC50 value of 0.364 μM.
- Jeong, Yunkyung,Lee, Jooyeon,Ryu, Jae-Sang
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supporting information
p. 2114 - 2124
(2016/04/20)
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- RING-TRANSFORMATIONS OF PYRIMIDINES BY INTRAMOLECULAR DIELS-ALDER REACTIONS. SYNTHESIS OF ANNELATED PYRIDINES
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Pyrimidines carrying an ω-alkyne side-chain -XCH2CH2CCH (X=O,N,S,SO,SO2) at the 2 or 5 position undergo intramolecular inverse electron demand Diels-Alder reactions across the C-2 and C-5 positions; elimination of hydrogen (or alkyl) cyanide from the intermediate adducts leads to condensed pyridines.The influence of the hetero atom (X) in the dienophilic side-chain and that of substituents in the pyrimidine ring on the reactivity is discussed.
- Frissen, A. E.,Marcelis, A. T. M.,Plas, H. C. van der
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p. 803 - 812
(2007/10/02)
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- NOVEL INTRAMOLECULAR DIELS-ALDER REACTIONS OF PYRIMIDINES. SYNTHESIS OF HETEROCYCLIC ANNELATED PYRIDINES
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Pyrimidines carrying a dienophilic side-chain at the 2 or 5 position undergo intramolecular Diels-Adler reactions to give heterocyclic annelated pyridines
- Frissen, August E.,Marcelis, Antonius T. M.,Plas, Henk C. van der
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p. 1589 - 1592
(2007/10/02)
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