33630-96-5Relevant academic research and scientific papers
Discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d[pyrimidine derivatives as potent Mnk inhibitors: Synthesis, structure-activity relationship analysis and biological evaluation
Yu, Mingfeng,Li, Peng,K.c. Basnet, Sunita,Kumarasiri, Malika,Diab, Sarah,Teo, Theodosia,Albrecht, Hugo,Wang, Shudong
, p. 116 - 126 (2015)
Phosphorylation of the eukaryotic initiation factor 4E (eIF4E) by mitogen-activated protein kinase (MAPK)-interacting kinases (Mnks) is essential for oncogenesis but unnecessary for normal development. Thus, pharmacological inhibition of Mnks may offer an effective and non-toxic anti-cancer therapeutic strategy. Herein, we report the discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d]pyrimidine derivatives as potent Mnk inhibitors. Docking study of 7a in Mnk2 suggests that the compound is stabilised in the ATP binding site through multiple hydrogen bonds and hydrophobic interaction. Cellular mechanistic studies on MV-4-11 cells with leads 7a, 8e and 8f reveal that they are able to down-regulate the phosphorylated eIF4E, Mcl-1 and cyclin D1, and induce apoptosis.
COMPOUNDS AND USES THEREOF
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Page/Page column 176, (2020/08/13)
The present invention features compounds useful in the treatment of neurological disorders and primary brain cancer. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders and primary brain cancer.
IMIDAZOPYRROLIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 89, (2014/12/12)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
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Page/Page column 32-33, (2012/04/23)
The new pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases especially against c-Met and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
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Page/Page column 47, (2010/01/12)
Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
ARYL-AMINO SUBSTITUTED PYRROLOPYRIMIDINE MULTI-KINASE INHIBITING COMPOUNDS
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Page/Page column 153, (2008/06/13)
Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3?, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2
5,7-DIAMINOPYRAZOLO`4,3-D!PYRIMIDINES USEFUL IN THE TREATMENT OF HYPERTENSION
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Page 217, (2008/06/13)
This invention relates to compounds of formula (I).
Chroman derivative and pharmaceutical use thereof
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, (2008/06/13)
Chroman derivatives of the formula ?I! STR1 wherein R1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R3 is a lower alkoxyalkyl or an aryloxyalkyl; R4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action. Accordingly, it is possible to selectively increase the coronary blood flow without causing a sudden hypotention causative of tachycardia which has a detrimental effect on the heart, and they are useful as a coronary vasodilator, in particular, an agent for the prophylaxis and treatment of cardiovascular disorders such as angina pectoris and heart failure.
REDUCTION OF HETERO-AROMATIC NITRO COMPOUNDS WITH BAKER'S YEAST
Takeshita, Mitsuhiro,Yoshida, Sachiko
, p. 2201 - 2204 (2007/10/02)
Reduction of nitro group on hetero-aromatics with baker's yeast has been examined.
Reaction with Acetic Anhydride as a Method for Estimating the Basicity of Exocyclic Amino Groups in Nitrogen Heterocycles
Deady, Leslie W.,Finlayson, Wayne L.
, p. 1625 - 1630 (2007/10/02)
Relative rates for acetylation of various anilines and amino heterocycles with acetic anhydride in pyridine were determined by a competition method.From a Broensted plot of reactivity against basicity for the anilines, and by considering the heterocycles as substituted anilines, pKa values for the amino group in a variety of heterocycles have been obtained.
