1364791-72-9Relevant academic research and scientific papers
4-Hydroxy-: N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade
Pippione, Agnese C.,Federico, Antonella,Ducime, Alex,Sainas, Stefano,Boschi, Donatella,Barge, Alessandro,Lupino, Elisa,Piccinini, Marco,Kubbutat, Michael,Contreras, Jean-Marie,Morice, Christophe,Al-Karadaghi, Salam,Lolli, Marco L.
, p. 1850 - 1855 (2017)
The NF-κB signaling pathway is a validated oncological target. Here, we applied scaffold hopping to IMD-0354, a presumed IKKβ inhibitor, and identified 4-hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide (4) as a nM-inhibitor of t
Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach
Pippione, Agnese C.,Giraudo, Alessandro,Bonanni, Davide,Carnovale, Irene M.,Marini, Elisabetta,Cena, Clara,Costale, Annalisa,Zonari, Daniele,Pors, Klaus,Sadiq, Maria,Boschi, Donatella,Oliaro-Bosso, Simonetta,Lolli, Marco L.
, p. 936 - 946 (2017/09/08)
The aldo-keto reductase 1C3 isoform (AKR1C3) plays a vital role in the biosynthesis of androgens, making this enzyme an attractive target for castration-resistant prostate cancer therapy. Although AKR1C3 is a promising drug target, no AKR1C3-targeted agen
New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold
Lolli, Marco L.,Giorgis, Marta,Tosco, Paolo,Foti, Antonio,Fruttero, Roberta,Gasco, Alberto
experimental part, p. 102 - 109 (2012/04/04)
Based on some structural analogies with leflunomide and brequinar, two well-known inhibitors of dihydroorotate dehydrogenase (DHODH), a new series of products was designed, by joining the substituted biphenyl moiety to the 4-hydroxy-1,2,5-oxadiazol-3-yl s
