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Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities.
Galdeano C, Gadd MS, Soares P, Scaffidi S, Van Molle I, Birced I, Hewitt S, Dias DM, Ciulli A. Galdeano C, et al. J Med Chem. 2014 Oct 23;57(20):8657-63. doi: 10.1021/jm5011258. Epub 2014 Oct 6. J Med Chem. 2014. PMID: 25166285 Free PMC article.
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. Soares P, et al. Among authors: galdeano c. J Med Chem. 2018 Jan 25;61(2):599-618. doi: 10.1021/acs.jmedchem.7b00675. Epub 2017 Sep 18. J Med Chem. 2018. PMID: 28853884 Free PMC article.
Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.
Galdeano C, Viayna E, Sola I, Formosa X, Camps P, Badia A, Clos MV, Relat J, Ratia M, Bartolini M, Mancini F, Andrisano V, Salmona M, Minguillón C, González-Muñoz GC, Rodríguez-Franco MI, Bidon-Chanal A, Luque FJ, Muñoz-Torrero D. Galdeano C, et al. J Med Chem. 2012 Jan 26;55(2):661-9. doi: 10.1021/jm200840c. Epub 2012 Jan 10. J Med Chem. 2012. PMID: 22185619
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
Camps P, Formosa X, Galdeano C, Muñoz-Torrero D, Ramírez L, Gómez E, Isambert N, Lavilla R, Badia A, Clos MV, Bartolini M, Mancini F, Andrisano V, Arce MP, Rodríguez-Franco MI, Huertas O, Dafni T, Luque FJ. Camps P, et al. Among authors: galdeano c. J Med Chem. 2009 Sep 10;52(17):5365-79. doi: 10.1021/jm900859q. J Med Chem. 2009. PMID: 19663388
Huprines as a new family of dual acting trypanocidal-antiplasmodial agents.
Defaux J, Sala M, Formosa X, Galdeano C, Taylor MC, Alobaid WA, Kelly JM, Wright CW, Camps P, Muñoz-Torrero D. Defaux J, et al. Among authors: galdeano c. Bioorg Med Chem. 2011 Mar 1;19(5):1702-7. doi: 10.1016/j.bmc.2011.01.028. Epub 2011 Jan 21. Bioorg Med Chem. 2011. PMID: 21315611 Free PMC article.
42 results