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Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds.
Sainas S, Pippione AC, Giorgis M, Lupino E, Goyal P, Ramondetti C, Buccinnà B, Piccinini M, Braga RC, Andrade CH, Andersson M, Moritzer AC, Friemann R, Mensa S, Al-Kadaraghi S, Boschi D, Lolli ML. Sainas S, et al. Among authors: boschi d. Eur J Med Chem. 2017 Mar 31;129:287-302. doi: 10.1016/j.ejmech.2017.02.017. Epub 2017 Feb 14. Eur J Med Chem. 2017. PMID: 28235702
Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
Pippione AC, Giraudo A, Bonanni D, Carnovale IM, Marini E, Cena C, Costale A, Zonari D, Pors K, Sadiq M, Boschi D, Oliaro-Bosso S, Lolli ML. Pippione AC, et al. Among authors: boschi d. Eur J Med Chem. 2017 Oct 20;139:936-946. doi: 10.1016/j.ejmech.2017.08.046. Epub 2017 Aug 24. Eur J Med Chem. 2017. PMID: 28881288 Free article.
Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid.
Pippione AC, Carnovale IM, Bonanni D, Sini M, Goyal P, Marini E, Pors K, Adinolfi S, Zonari D, Festuccia C, Wahlgren WY, Friemann R, Bagnati R, Boschi D, Oliaro-Bosso S, Lolli ML. Pippione AC, et al. Among authors: boschi d. Eur J Med Chem. 2018 Apr 25;150:930-945. doi: 10.1016/j.ejmech.2018.03.040. Epub 2018 Mar 16. Eur J Med Chem. 2018. PMID: 29602039
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.
Sainas S, Pippione AC, Lupino E, Giorgis M, Circosta P, Gaidano V, Goyal P, Bonanni D, Rolando B, Cignetti A, Ducime A, Andersson M, Järvå M, Friemann R, Piccinini M, Ramondetti C, Buccinnà B, Al-Karadaghi S, Boschi D, Saglio G, Lolli ML. Sainas S, et al. Among authors: boschi d. J Med Chem. 2018 Jul 26;61(14):6034-6055. doi: 10.1021/acs.jmedchem.8b00373. Epub 2018 Jul 9. J Med Chem. 2018. PMID: 29939742
62 results