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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: ardini e. Chirality. 2022 Nov;34(11):1437-1452. doi: 10.1002/chir.23501. Epub 2022 Aug 12. Chirality. 2022. PMID: 35959859
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: ardini 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
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
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. Among authors: ardini e. 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
The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition.
Ardini E, Bosotti R, Borgia AL, De Ponti C, Somaschini A, Cammarota R, Amboldi N, Raddrizzani L, Milani A, Magnaghi P, Ballinari D, Casero D, Gasparri F, Banfi P, Avanzi N, Saccardo MB, Alzani R, Bandiera T, Felder E, Donati D, Pesenti E, Sartore-Bianchi A, Gambacorta M, Pierotti MA, Siena S, Veronese S, Galvani A, Isacchi A. Ardini E, et al. Mol Oncol. 2014 Dec;8(8):1495-507. doi: 10.1016/j.molonc.2014.06.001. Epub 2014 Jun 12. Mol Oncol. 2014. PMID: 24962792 Free PMC article.
ALK Inhibitors, a Pharmaceutical Perspective.
Ardini E, Galvani A. Ardini E, et al. Front Oncol. 2012 Feb 22;2:17. doi: 10.3389/fonc.2012.00017. eCollection 2012. Front Oncol. 2012. PMID: 22655263 Free PMC article.
Sensitivity to Entrectinib Associated With a Novel LMNA-NTRK1 Gene Fusion in Metastatic Colorectal Cancer.
Sartore-Bianchi A, Ardini E, Bosotti R, Amatu A, Valtorta E, Somaschini A, Raddrizzani L, Palmeri L, Banfi P, Bonazzina E, Misale S, Marrapese G, Leone A, Alzani R, Luo D, Hornby Z, Lim J, Veronese S, Vanzulli A, Bardelli A, Martignoni M, Davite C, Galvani A, Isacchi A, Siena S. Sartore-Bianchi A, et al. Among authors: ardini e. J Natl Cancer Inst. 2015 Nov 12;108(1):djv306. doi: 10.1093/jnci/djv306. Print 2016 Jan. J Natl Cancer Inst. 2015. PMID: 26563355 Free PMC article.
32 results