72965-16-3Relevant academic research and scientific papers
Identification of the first small-molecule inhibitor of the REV7 DNA repair protein interaction
Actis, Marcelo L.,Ambaye, Nigus D.,Evison, Benjamin J.,Shao, Youming,Vanarotti, Murugendra,Inoue, Akira,McDonald, Ezelle T.,Kikuchi, Sotaro,Heath, Richard,Hara, Kodai,Hashimoto, Hiroshi,Fujii, Naoaki
supporting information, p. 4339 - 4346 (2016/08/23)
DNA interstrand crosslink (ICL) repair (ICLR) has been implicated in the resistance of cancer cells to ICL-inducing chemotherapeutic agents. Despite the clinical significance of ICL-inducing chemotherapy, few studies have focused on developing small-molec
Synthesis and structure of some thienopyrimidine derivatives
Hamed, Atef A.,Zeid, Ibrahim F.,El-Ganzory, Hussein H.,Abdel Aal, Mohamed T.
experimental part, p. 809 - 820 (2009/09/06)
A series of substituted thieno[2,3-d]pyrimidines was synthesized starting from ethyl-2-amino-4-isopropylthiophene-3-carboxlate. Reaction of 2-hydrazino-5-isopropyl-thieno[2,3-d]pyrimidin-4(3H)-one and its 3-methyl analogue with different reagents afforded thieno[2,3-d]triazolo[4,3-a] pyrimidines and thieno[3,2-e]triazolo[4,3-a]pyrimidines, beside open chain derivatives.
SUBSTITUED 3,4-DIHYDROTHIENO [2,3-D] PYRMIDINES AS TISSUE TRANSGLUTAMINASE INHIBITORS
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Page/Page column 50; 52, (2010/11/08)
The present invention provides novel compounds and methods useful for treating transglutaminase associated disorders such as celiac spru, Alzheimer's disease and Huntington's disease. Certain compounds of the invention are tissue transglutaminase inhibito
Structure-activity relationship study of novel tissue transglutaminase inhibitors
Duval, Eric,Case, April,Stein, Ross L.,Cuny, Gregory D.
, p. 1885 - 1889 (2007/10/03)
Thieno[2,3-d]pyrimidin-4-one acylhydrazide derivatives were discovered as moderately potent inhibitors of TGase 2 (tissue transglutaminase) utilizing a fluorescence-based assay that measured TGase 2 catalyzed incorporation of the dansylated Lys derivative
2-(Diethylamino)thieno[1,3]oxazin-4-ones as stable inhibitors of human leukocyte elastase
Gütschow, Michael,Kuerschner, Lars,Neumann, Ulf,Pietsch, Markus,L?ser, Reik,Koglin, Norman,Eger, Kurt
, p. 5437 - 5447 (2007/10/03)
A series of 2-(diethylamino)thieno[1,3]oxazin-4-ones was synthesized and evaluated in vitro for inhibitory activity toward human leukocyte elastase (HLE). The Gewald thiophene synthesis was utilized to obtain several ethyl 2-aminothiophene-3- carboxylates. These precursors were subjected to a five-step route to obtain thieno[2,3-d][1,3]oxazin-4-ones bearing various substituents at positions 5 and 6. Both thieno[2,3-d] and thieno[3,2-d] fused oxazin-4-ones possess extraordinary chemical stability, which was expressed as rate constants of the alkaline hydrolysis. The kinetic parameters of the HLE inhibition were determined. The most potent compound, 2-(diethylamino)-4H- [1]benzothieno[2,3-d][1,3]oxazin-4-one, exhibited a K(i) value of 5.8 nM. 2-(Diethylamino)thieno[1,3]oxazin-4-ones act as acyl- enzyme inhibitors of HLE, similar to the inhibition of serine proteases by 4H-3,1-benzoxazin-4-ones. The isosteric benzene- thiophene replacement accounts for an enhanced stability of the acyl-enzyme intermediates.
Thieno pyrazine diones, their preparation and use
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, (2008/06/13)
Novel thieno[2,3-b]pyrazine-2,3(1H,3H)-diones or tautomeric forms thereof of the formula (I) STR1 The compounds are useful in the treatment of neurological and psychiatric diseases.
