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Page 1
The target landscape of clinical kinase drugs.
Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B. Klaeger S, et al. Among authors: felder er. Science. 2017 Dec 1;358(6367):eaan4368. doi: 10.1126/science.aan4368. Science. 2017. PMID: 29191878 Free PMC article.
Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids.
Casuscelli F, Ardini E, Avanzi N, Badari A, Casale E, Disingrini T, Donati D, Ermoli A, Felder ER, Galvani A, Isacchi A, Menichincheri M, Montemartini M, Orrenius C, Piutti C, Salom B, Papeo G. Casuscelli F, et al. Among authors: felder er. Chirality. 2022 Nov;34(11):1437-1452. doi: 10.1002/chir.23501. Epub 2022 Aug 12. Chirality. 2022. PMID: 35959859
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
NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.
Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A. Fogliatto G, et al. Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14. Clin Cancer Res. 2013. PMID: 23674492
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
Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.
Brasca MG, Gnocchi P, Nesi M, Amboldi N, Avanzi N, Bertrand J, Bindi S, Canevari G, Casero D, Ciomei M, Colombo N, Cribioli S, Fachin G, Felder ER, Galvani A, Isacchi A, Motto I, Panzeri A, Donati D. Brasca MG, et al. Among authors: felder er. Bioorg Med Chem. 2015 May 15;23(10):2387-407. doi: 10.1016/j.bmc.2015.03.059. Epub 2015 Mar 28. Bioorg Med Chem. 2015. PMID: 25882525
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
Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications.
Ardini E, Menichincheri M, Banfi P, Bosotti R, De Ponti C, Pulci R, Ballinari D, Ciomei M, Texido G, Degrassi A, Avanzi N, Amboldi N, Saccardo MB, Casero D, Orsini P, Bandiera T, Mologni L, Anderson D, Wei G, Harris J, Vernier JM, Li G, Felder E, Donati D, Isacchi A, Pesenti E, Magnaghi P, Galvani A. Ardini E, et al. Mol Cancer Ther. 2016 Apr;15(4):628-39. doi: 10.1158/1535-7163.MCT-15-0758. Epub 2016 Mar 3. Mol Cancer Ther. 2016. PMID: 26939704
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
75 results