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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: di fruscia p. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Fragment-Based Discovery of Novel Allosteric MEK1 Binders.
Di Fruscia P, Edfeldt F, Shamovsky I, Collie GW, Aagaard A, Barlind L, Börjesson U, Hansson EL, Lewis RJ, Nilsson MK, Öster L, Pemberton J, Ripa L, Storer RI, Käck H. Di Fruscia P, et al. ACS Med Chem Lett. 2021 Jan 27;12(2):302-308. doi: 10.1021/acsmedchemlett.0c00563. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603979 Free PMC article.
Put a ring on it: application of small aliphatic rings in medicinal chemistry.
Bauer MR, Di Fruscia P, Lucas SCC, Michaelides IN, Nelson JE, Storer RI, Whitehurst BC. Bauer MR, et al. Among authors: di fruscia p. RSC Med Chem. 2021 Jan 7;12(4):448-471. doi: 10.1039/d0md00370k. eCollection 2021 Apr 28. RSC Med Chem. 2021. PMID: 33937776 Free PMC article. Review.
Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-Covalent N-Acylethanolamine-Hydrolyzing Acid Amidase (NAAA) Inhibitors for Oral Administration.
Di Fruscia P, Carbone A, Bottegoni G, Berti F, Giacomina F, Ponzano S, Pagliuca C, Fiasella A, Pizzirani D, Ortega JA, Nuzzi A, Tarozzo G, Mengatto L, Giampà R, Penna I, Russo D, Romeo E, Summa M, Bertorelli R, Armirotti A, Bertozzi SM, Reggiani A, Bandiera T, Bertozzi F. Di Fruscia P, et al. J Med Chem. 2021 Sep 23;64(18):13327-13355. doi: 10.1021/acs.jmedchem.1c00575. Epub 2021 Sep 1. J Med Chem. 2021. PMID: 34469137 Free PMC article.
Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators.
Brindani N, Gianotti A, Giovani S, Giacomina F, Di Fruscia P, Sorana F, Bertozzi SM, Ottonello G, Goldoni L, Penna I, Russo D, Summa M, Bertorelli R, Ferrera L, Pesce E, Sondo E, Galietta LJV, Bandiera T, Pedemonte N, Bertozzi F. Brindani N, et al. Among authors: di fruscia p. J Med Chem. 2020 Oct 8;63(19):11169-11194. doi: 10.1021/acs.jmedchem.0c01050. Epub 2020 Sep 18. J Med Chem. 2020. PMID: 32946228 Free PMC article.
The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model.
Di Fruscia P, Zacharioudakis E, Liu C, Moniot S, Laohasinnarong S, Khongkow M, Harrison IF, Koltsida K, Reynolds CR, Schmidtkunz K, Jung M, Chapman KL, Steegborn C, Dexter DT, Sternberg MJ, Lam EW, Fuchter MJ. Di Fruscia P, et al. ChemMedChem. 2015 Jan;10(1):69-82. doi: 10.1002/cmdc.201402431. Epub 2014 Nov 13. ChemMedChem. 2015. PMID: 25395356
The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors.
Di Fruscia P, Ho KK, Laohasinnarong S, Khongkow M, Kroll SH, Islam SA, Sternberg MJ, Schmidtkunz K, Jung M, Lam EW, Fuchter MJ. Di Fruscia P, et al. Medchemcomm. 2012 Mar 1;(3):10.1039/C2MD00290F. doi: 10.1039/C2MD00290F. Medchemcomm. 2012. PMID: 24340169 Free PMC article.
14 results