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16 results

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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. Among authors: pastori w. ChemMedChem. 2015 Feb;10(2):276-95. doi: 10.1002/cmdc.201402424. Epub 2014 Nov 27. ChemMedChem. 2015. PMID: 25430902
6-Substituted pyrrolo[3,4-c]pyrazoles: an improved class of CDK2 inhibitors.
Brasca MG, Albanese C, Amici R, Ballinari D, Corti L, Croci V, Fancelli D, Fiorentini F, Nesi M, Orsini P, Orzi F, Pastori W, Perrone E, Pesenti E, Pevarello P, Riccardi-Sirtori F, Roletto F, Roussel P, Varasi M, Vulpetti A, Mercurio C. Brasca MG, et al. Among authors: pastori w. ChemMedChem. 2007 Jun;2(6):841-52. doi: 10.1002/cmdc.200600302. ChemMedChem. 2007. PMID: 17450625
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA. Pevarello P, et al. Among authors: pastori w. J Med Chem. 2004 Jun 17;47(13):3367-80. doi: 10.1021/jm031145u. J Med Chem. 2004. PMID: 15189033
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.
Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C. Pevarello P, et al. Among authors: pastori w. J Med Chem. 2005 Apr 21;48(8):2944-56. doi: 10.1021/jm0408870. J Med Chem. 2005. PMID: 15828833
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: pastori w. 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: pastori w. 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
Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.
Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M. Albanese C, et al. Among authors: pastori w. Mol Cancer Ther. 2010 Aug;9(8):2243-54. doi: 10.1158/1535-7163.MCT-10-0190. Epub 2010 Aug 3. Mol Cancer Ther. 2010. PMID: 20682657
Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers.
Modugno M, Banfi P, Gasparri F, Borzilleri R, Carter P, Cornelius L, Gottardis M, Lee V, Mapelli C, Naglich JG, Tebben A, Vite G, Pastori W, Albanese C, Corti E, Ballinari D, Galvani A. Modugno M, et al. Among authors: pastori w. Exp Cell Res. 2015 Mar 15;332(2):267-77. doi: 10.1016/j.yexcr.2014.11.022. Epub 2014 Dec 5. Exp Cell Res. 2015. PMID: 25486070
16 results