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Schnekenburger, Michael,Goffin, Eric,Lee, Jin-Young,Jang, Jun Young,Mazumder, Aloran,Ji, Seungwon,Rogister, Bernard,Bouider, Nafila,Lefranc, Florence,Miklos, Walter,Mathieu, Vé,ronique,de Tullio American Chemical Society 2017 Journal of medicinal chemistry Vol.60 No.11
<P>A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. On the basis of computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-3-cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea] which displays a potent anti.proliferative activity on various glioma cell types, assessed by quantitative videomicroscopy, eventually triggering senescence. The impact on normal glial cells was lower with a selectivity index of >10. Furthermore, human U373 and Hs683 glioblastoma cell lines served to demonstrate the inhibitory activity of 18 against histone deacetylase (HDAC) class III sirtuins 1 and 2 (SIRT1/2) by quantifying acetylation levels of histone and non-histone proteins. The translational potential of 18 was validated by an NCI-60 cell line screen and validation of growth inhibition of drug resistant cancer cell models. Eventually, the anticancer potential of 18 was validated- in 3D glioblastoma spheroids and in vivo by zebrafish xenografts. In summary, compound 18 is the first representative of a new class of SIRT inhibitors opening new perspectives in the medicinal chemistry of HDAC inhibitors.</P>
Safety and efficiency of molnupiravir for COVID-19 patients with advanced chronic kidney disease
( Inès Dufour ),( Arnaud Devresse ),( Anais Scohy ),( Caroline Briquet ),( Hélène Georgery ),( Philippe Delaey ),( Julien De Greef ),( Eric Goffin ),( Laura Labriola ) 대한신장학회 2023 Kidney Research and Clinical Practice Vol.42 No.2
ISPD Peritonitis Recommendations: 2016 Update on Prevention and Treatment
Li, Philip Kam-Tao,Szeto, Cheuk Chun,Piraino, Beth,de Arteaga, Javier,Fan, Stanley,Figueiredo, Ana E.,Fish, Douglas N.,Goffin, Eric,Kim, Yong-Lim,Salzer, William,Struijk, Dirk G.,Teitelbaum, Isaac,Joh Multimed Inc 2016 Peritoneal dialysis international Vol.36 No.5