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New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold.
Pippione AC, Kilic-Kurt Z, Kovachka S, Sainas S, Rolando B, Denasio E, Pors K, Adinolfi S, Zonari D, Bagnati R, Lolli ML, Spyrakis F, Oliaro-Bosso S, Boschi D. Pippione AC, et al. Eur J Med Chem. 2022 Jul 5;237:114366. doi: 10.1016/j.ejmech.2022.114366. Epub 2022 Apr 13. Eur J Med Chem. 2022. PMID: 35447434 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. 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 Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold: SAR of the Biphenyl Moiety.
Sainas S, Giorgis M, Circosta P, Gaidano V, Bonanni D, Pippione AC, Bagnati R, Passoni A, Qiu Y, Cojocaru CF, Canepa B, Bona A, Rolando B, Mishina M, Ramondetti C, Buccinnà B, Piccinini M, Houshmand M, Cignetti A, Giraudo E, Al-Karadaghi S, Boschi D, Saglio G, Lolli ML. Sainas S, et al. Among authors: pippione ac. J Med Chem. 2021 May 13;64(9):5404-5428. doi: 10.1021/acs.jmedchem.0c01549. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844533 Free PMC article.
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold: SAR of the Aryloxyaryl Moiety.
Sainas S, Giorgis M, Circosta P, Poli G, Alberti M, Passoni A, Gaidano V, Pippione AC, Vitale N, Bonanni D, Rolando B, Cignetti A, Ramondetti C, Lanno A, Ferraris DM, Canepa B, Buccinnà B, Piccinini M, Rizzi M, Saglio G, Al-Karadaghi S, Boschi D, Miggiano R, Tuccinardi T, Lolli ML. Sainas S, et al. Among authors: pippione ac. J Med Chem. 2022 Oct 13;65(19):12701-12724. doi: 10.1021/acs.jmedchem.2c00496. Epub 2022 Sep 26. J Med Chem. 2022. PMID: 36162075 Free PMC article.
Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies.
Pippione AC, Sainas S, Goyal P, Fritzson I, Cassiano GC, Giraudo A, Giorgis M, Tavella TA, Bagnati R, Rolando B, Caing-Carlsson R, Costa FTM, Andrade CH, Al-Karadaghi S, Boschi D, Friemann R, Lolli ML. Pippione AC, et al. Eur J Med Chem. 2019 Feb 1;163:266-280. doi: 10.1016/j.ejmech.2018.11.044. Epub 2018 Nov 22. Eur J Med Chem. 2019. PMID: 30529545 Free article.
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. Among authors: pippione ac. 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.
AKR1C3 is a biomarker and druggable target for oropharyngeal tumors.
Peraldo-Neia C, Ostano P, Mello-Grand M, Guana F, Gregnanin I, Boschi D, Oliaro-Bosso S, Pippione AC, Carenzo A, De Cecco L, Cavalieri S, Micali A, Perrone F, Averono G, Bagnasacco P, Dosdegani R, Masini L, Krengli M, Aluffi-Valletti P, Valente G, Chiorino G. Peraldo-Neia C, et al. Among authors: pippione ac. Cell Oncol (Dordr). 2021 Apr;44(2):357-372. doi: 10.1007/s13402-020-00571-z. Epub 2020 Nov 19. Cell Oncol (Dordr). 2021. PMID: 33211282
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: pippione ac. 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
24 results