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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: lolli ml. 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: lolli ml. 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
Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3.
Lolli ML, Carnovale IM, Pippione AC, Wahlgren WY, Bonanni D, Marini E, Zonari D, Gallicchio M, Boscaro V, Goyal P, Friemann R, Rolando B, Bagnati R, Adinolfi S, Oliaro-Bosso S, Boschi D. Lolli ML, et al. ACS Med Chem Lett. 2019 Jan 28;10(4):437-443. doi: 10.1021/acsmedchemlett.8b00484. eCollection 2019 Apr 11. ACS Med Chem Lett. 2019. PMID: 30996776 Free PMC article.
A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action.
Campaner E, Rustighi A, Zannini A, Cristiani A, Piazza S, Ciani Y, Kalid O, Golan G, Baloglu E, Shacham S, Valsasina B, Cucchi U, Pippione AC, Lolli ML, Giabbai B, Storici P, Carloni P, Rossetti G, Benvenuti F, Bello E, D'Incalci M, Cappuzzello E, Rosato A, Del Sal G. Campaner E, et al. Among authors: lolli ml. Nat Commun. 2017 Jun 9;8:15772. doi: 10.1038/ncomms15772. Nat Commun. 2017. PMID: 28598431 Free PMC article.
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML. Sainas S, et al. Among authors: lolli ml. J Med Chem. 2019 May 9;62(9):4467-4482. doi: 10.1021/acs.jmedchem.8b01986. Epub 2019 Apr 18. J Med Chem. 2019. PMID: 30943028 Free PMC article.
71 results