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Page 1
Optimization of diarylthiazole B-raf inhibitors: identification of a compound endowed with high oral antitumor activity, mitigated hERG inhibition, and low paradoxical effect.
Pulici M, Traquandi G, Marchionni C, Modugno M, Lupi R, Amboldi N, Casale E, Colombo N, Corti L, Fasolini M, Gasparri F, Pastori W, Scolaro A, Donati D, Felder E, Galvani A, Isacchi A, Pesenti E, Ciomei M. Pulici M, et al. ChemMedChem. 2015 Feb;10(2):276-95. doi: 10.1002/cmdc.201402424. Epub 2014 Nov 27. ChemMedChem. 2015. PMID: 25430902
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: felder er. 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
Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors.
Cervi G, Magnaghi P, Asa D, Avanzi N, Badari A, Borghi D, Caruso M, Cirla A, Cozzi L, Felder E, Galvani A, Gasparri F, Lomolino A, Magnuson S, Malgesini B, Motto I, Pasi M, Rizzi S, Salom B, Sorrentino G, Troiani S, Valsasina B, O'Brien T, Isacchi A, Donati D, D'Alessio R. Cervi G, et al. J Med Chem. 2014 Dec 26;57(24):10443-54. doi: 10.1021/jm501313x. Epub 2014 Dec 12. J Med Chem. 2014. PMID: 25474526
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.
Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P. Menichincheri M, et al. J Med Chem. 2016 Apr 14;59(7):3392-408. doi: 10.1021/acs.jmedchem.6b00064. Epub 2016 Mar 30. J Med Chem. 2016. PMID: 27003761
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M, Fasolini M, Forte B, Galvani A, Isacchi A, Khvat A, Krasavin MY, Lupi R, Orsini P, Perego R, Pesenti E, Pezzetta D, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Sola F, Zuccotto F, Felder ER, Donati D, Montagnoli A. Papeo G, et al. Among authors: felder er. J Med Chem. 2015 Sep 10;58(17):6875-98. doi: 10.1021/acs.jmedchem.5b00680. Epub 2015 Aug 26. J Med Chem. 2015. PMID: 26222319
Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.
Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D. Brasca MG, et al. Among authors: felder er. Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21. Bioorg Med Chem. 2014. PMID: 25009002
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: felder er. 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
75 results