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Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7.
Zoppi V, Hughes SJ, Maniaci C, Testa A, Gmaschitz T, Wieshofer C, Koegl M, Riching KM, Daniels DL, Spallarossa A, Ciulli A. Zoppi V, et al. Among authors: spallarossa a. J Med Chem. 2019 Jan 24;62(2):699-726. doi: 10.1021/acs.jmedchem.8b01413. Epub 2018 Dec 28. J Med Chem. 2019. PMID: 30540463 Free PMC article.
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.
Ranise A, Spallarossa A, Schenone S, Bruno O, Bondavalli F, Vargiu L, Marceddu T, Mura M, La Colla P, Pani A. Ranise A, et al. Among authors: spallarossa a. J Med Chem. 2003 Feb 27;46(5):768-81. doi: 10.1021/jm0209984. J Med Chem. 2003. PMID: 12593657
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
Ranise A, Spallarossa A, Cesarini S, Bondavalli F, Schenone S, Bruno O, Menozzi G, Fossa P, Mosti L, La Colla M, Sanna G, Murreddu M, Collu G, Busonera B, Marongiu ME, Pani A, La Colla P, Loddo R. Ranise A, et al. Among authors: spallarossa a. J Med Chem. 2005 Jun 2;48(11):3858-73. doi: 10.1021/jm049252r. J Med Chem. 2005. PMID: 15916438
Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.
Manetti F, Santucci A, Locatelli GA, Maga G, Spreafico A, Serchi T, Orlandini M, Bernardini G, Caradonna NP, Spallarossa A, Brullo C, Schenone S, Bruno O, Ranise A, Bondavalli F, Hoffmann O, Bologna M, Angelucci A, Botta M. Manetti F, et al. Among authors: spallarossa a. J Med Chem. 2007 Nov 15;50(23):5579-88. doi: 10.1021/jm061449r. Epub 2007 Oct 11. J Med Chem. 2007. PMID: 17929792
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Spallarossa A, Cesarini S, Ranise A, Schenone S, Bruno O, Borassi A, La Colla P, Pezzullo M, Sanna G, Collu G, Secci B, Loddo R. Spallarossa A, et al. Eur J Med Chem. 2009 May;44(5):2190-201. doi: 10.1016/j.ejmech.2008.10.032. Epub 2008 Nov 5. Eur J Med Chem. 2009. PMID: 19058881
6-amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives as a new class of potent inhibitors of Interleukin-8-induced neutrophil chemotaxis.
Cesarini S, Spallarossa A, Ranise A, Bruno O, Arduino N, Bertolotto M, Dallegri F, Tognolini M, Gobbetti T, Barocelli E. Cesarini S, et al. Among authors: spallarossa a. Bioorg Med Chem. 2009 May 15;17(10):3580-7. doi: 10.1016/j.bmc.2009.04.006. Epub 2009 Apr 11. Bioorg Med Chem. 2009. PMID: 19394230
66 results