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Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer.
Pippione AC, Kovachka S, Vigato C, Bertarini L, Mannella I, Sainas S, Rolando B, Denasio E, Piercy-Mycock H, Romalho L, Salladini E, Adinolfi S, Zonari D, Peraldo-Neia C, Chiorino G, Passoni A, Mirza OA, Frydenvang K, Pors K, Lolli ML, Spyrakis F, Oliaro-Bosso S, Boschi D. Pippione AC, et al. Among authors: pors k. Eur J Med Chem. 2024 Mar 15;268:116193. doi: 10.1016/j.ejmech.2024.116193. Epub 2024 Feb 7. Eur J Med Chem. 2024. PMID: 38364714 Free article.
Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties.
Cosentino L, Redondo-Horcajo M, Zhao Y, Santos AR, Chowdury KF, Vinader V, Abdallah QM, Abdel-Rahman H, Fournier-Dit-Chabert J, Shnyder SD, Loadman PM, Fang WS, Díaz JF, Barasoain I, Burns PA, Pors K. Cosentino L, et al. Among authors: pors k. J Med Chem. 2012 Dec 27;55(24):11062-6. doi: 10.1021/jm301151t. Epub 2012 Dec 7. J Med Chem. 2012. PMID: 23176628
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: pors k. 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: pors k. 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
Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo-keto reductase 1C3 target affinity.
Santos ARN, Sheldrake HM, Ibrahim AIM, Danta CC, Bonanni D, Daga M, Oliaro-Bosso S, Boschi D, Lolli ML, Pors K. Santos ARN, et al. Among authors: pors k. Medchemcomm. 2019 Jun 27;10(8):1476-1480. doi: 10.1039/c9md00201d. eCollection 2019 Aug 1. Medchemcomm. 2019. PMID: 31673310 Free PMC article.
Expansion of the 4-(Diethylamino)benzaldehyde Scaffold to Explore the Impact on Aldehyde Dehydrogenase Activity and Antiproliferative Activity in Prostate Cancer.
Ibrahim AIM, Batlle E, Sneha S, Jiménez R, Pequerul R, Parés X, Rüngeler T, Jha V, Tuccinardi T, Sadiq M, Frame F, Maitland NJ, Farrés J, Pors K. Ibrahim AIM, et al. Among authors: pors k. J Med Chem. 2022 Mar 10;65(5):3833-3848. doi: 10.1021/acs.jmedchem.1c01367. Epub 2022 Feb 25. J Med Chem. 2022. PMID: 35212533 Free PMC article.
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. Among authors: pors k. 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.
Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation.
Fournier-Dit-Chabert J, Vinader V, Santos AR, Redondo-Horcajo M, Dreneau A, Basak R, Cosentino L, Marston G, Abdel-Rahman H, Loadman PM, Shnyder SD, Díaz JF, Barasoain I, Falconer RA, Pors K. Fournier-Dit-Chabert J, et al. Among authors: pors k. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7693-6. doi: 10.1016/j.bmcl.2012.09.104. Epub 2012 Oct 10. Bioorg Med Chem Lett. 2012. PMID: 23103097
61 results