14103-22-1Relevant articles and documents
Selective reduction of the endocyclic double bond of 3-substituted coumarins by hantzsch 1,4-dihydropyridine
Liu, Zhengang,Liu, Qiang,Zhang, Wei,Mu, Ruizhu,Yang, Li,Liu, Zhong-Li,Yu, Wei
, p. 771 - 774 (2006)
Hantzsch 1,4-dihydropyridine is a valuable reagent to effect the chemoselective reduction of the 3,4-double bond of 3-substituted coumarins. Georg Thieme Verlag Stuttgart.
Development of pyrazolone and isoxazol-5-one cambinol analogues as sirtuin inhibitors
Mahajan, Sumit S.,Scian, Michele,Sripathy, Smitha,Posakony, Jeff,Lao, Uyen,Loe, Taylor K.,Leko, Vid,Thalhofer, Angel,Schuler, Aaron D.,Bedalov, Antonio,Simon, Julian A.
, p. 3283 - 3294 (2014/05/20)
Sirtuins are a family of NAD+-dependent protein deacetylases that play critical roles in epigenetic regulation, stress responses, and cellular aging in eukaryotic cells. In an effort to identify small molecule inhibitors of sirtuins for potential use as chemotherapeutics as well as tools to modulate sirtuin activity, we previously identified a nonselective sirtuin inhibitor called cambinol (IC50 ≈ 50 μM for SIRT1 and SIRT2) with in vitro and in vivo antilymphoma activity. In the current study, we used saturation transfer difference (STD) NMR experiments with recombinant SIRT1 and 20 to map parts of the inhibitor that interacted with the protein. Our ongoing efforts to optimize cambinol analogues for potency and selectivity have resulted in the identification of isoform selective analogues: 17 with >7.8-fold selectivity for SIRT1, 24 with >15.4-fold selectivity for SIRT2, and 8 with 6.8- and 5.3-fold selectivity for SIRT3 versus SIRT1 and SIRT2, respectively. In vitro cytotoxicity studies with these compounds as well as EX527, a potent and selective SIRT1 inhibitor, suggest that antilymphoma activity of this compound class may be predominantly due to SIRT2 inhibition.
PYRIMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page/Page column 21, (2010/04/27)
The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar' is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alk
