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Page 1
Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships.
Polucci P, Magnaghi P, Angiolini M, Asa D, Avanzi N, Badari A, Bertrand J, Casale E, Cauteruccio S, Cirla A, Cozzi L, Galvani A, Jackson PK, Liu Y, Magnuson S, Malgesini B, Nuvoloni S, Orrenius C, Sirtori FR, Riceputi L, Rizzi S, Trucchi B, O'Brien T, Isacchi A, Donati D, D'Alessio R. Polucci P, et al. Among authors: casale e. J Med Chem. 2013 Jan 24;56(2):437-50. doi: 10.1021/jm3013213. Epub 2013 Jan 4. J Med Chem. 2013. PMID: 23245311
Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death.
Magnaghi P, D'Alessio R, Valsasina B, Avanzi N, Rizzi S, Asa D, Gasparri F, Cozzi L, Cucchi U, Orrenius C, Polucci P, Ballinari D, Perrera C, Leone A, Cervi G, Casale E, Xiao Y, Wong C, Anderson DJ, Galvani A, Donati D, O'Brien T, Jackson PK, Isacchi A. Magnaghi P, et al. Among authors: casale e. Nat Chem Biol. 2013 Sep;9(9):548-56. doi: 10.1038/nchembio.1313. Epub 2013 Jul 28. Nat Chem Biol. 2013. PMID: 23892893
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G. Brasca MG, et al. Among authors: casale e. Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19. Bioorg Med Chem. 2013. PMID: 24100158
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Casuscelli F, Ardini E, Avanzi N, Casale E, Cervi G, D'Anello M, Donati D, Faiardi D, Ferguson RD, Fogliatto G, Galvani A, Marsiglio A, Mirizzi DG, Montemartini M, Orrenius C, Papeo G, Piutti C, Salom B, Felder ER. Casuscelli F, et al. Among authors: casale e. Bioorg Med Chem. 2013 Dec 1;21(23):7364-80. doi: 10.1016/j.bmc.2013.09.054. Epub 2013 Oct 2. Bioorg Med Chem. 2013. PMID: 24139169
Identification of unprecedented ATP-competitive choline kinase inhibitors.
Quartieri F, Nesi M, Avanzi NR, Borghi D, Casale E, Corti E, Cucchi U, Donati D, Fasolini M, Felder ER, Galvani A, Giorgini ML, Lomolino A, Menichincheri M, Orrenius C, Perrera C, Re Depaolini S, Riccardi-Sirtori F, Salsi E, Isacchi A, Gnocchi P. Quartieri F, et al. Among authors: casale e. Bioorg Med Chem Lett. 2021 Nov 1;51:128310. doi: 10.1016/j.bmcl.2021.128310. Epub 2021 Aug 18. Bioorg Med Chem Lett. 2021. PMID: 34416377
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.
Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M. Brasca MG, et al. Among authors: casale e. J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559. J Med Chem. 2009. PMID: 19603809
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M. Brasca MG, et al. Among authors: casale e. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25. Bioorg Med Chem. 2010. PMID: 20153204
74 results