Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Giovanna Pescatore"'
Autor:
Fabrizio Fiore, Michael Rowley, Philip Jones, Odalys Gonzalez Paz, Massimiliano Fonsi, Edith Monteagudo, Olaf Kinzel, Carsten Schultz-Fademrecht, Christian Steinkühler, Giovanna Pescatore, Laura Llauger-Bufi
Publikováno v:
Journal of Medicinal Chemistry. 52:3453-3456
The optimization of a potent, class I selective ketone HDAC inhibitor is shown. It possesses optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, and is negative in a microbial mutagenicity (Ames) test. In a mo
Autor:
Christian Steinkühler, Fabrizio Fiore, Olaf Kinzel, Barbara Attenni, Sergio Serafini, Giovanna Pescatore, Ottavia Cecchetti, Carsten Schultz-Fademrecht, Massimiliano Fonsi, Michael Rowley, Philip Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5528-5532
Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in the clinic. Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading
Publikováno v:
Tetrahedron Letters. 44:6999-7002
Peptidic aminopeptidase inhibitors, bestatin, phebestin and probestin have been prepared by stereo- and regiocontrolled reactions from a common α,β-epoxy ester precursor.
Publikováno v:
Tetrahedron. 57:5649-5656
The results obtained in the MgBr2-mediated opening of 2,3-bifunctionalized epoxides are reported. The studies showed that the chelation control of MgBr2 between different functionalities can in some cases be selective.
Autor:
Giovanna Pescatore, et al. et al.
Publikováno v:
ChemInform. 41
Publikováno v:
ChemInform. 32
The results obtained in the MgBr2-mediated opening of 2,3-bifunctionalized epoxides are reported. The studies showed that the chelation control of MgBr2 between different functionalities can in some cases be selective.
Autor:
Carlo Toniatti, Fabrizio Fiore, Philip Jones, Laura Llauger Bufi, Danila Branca, Olaf Kinzel, Michael Rowley, Giovanna Pescatore, Caterina Torrisi, Ester Muraglia, Federica Orvieto
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(3)
Herein we describe the discovery of a novel series of pyrrolo[1,2-a]pyrazin-1(2H)-one PARP inhibitors. Optimization led to compounds that display excellent PARP-1 enzyme potency and inhibit the proliferation of BRCA deficient cells in the low double-
Autor:
Giovanna Pescatore, Samuele Lillini, Caterina Torrisi, Olaf Kinzel, Philip Jones, Costanza Bergami, Laura Llauger
Publikováno v:
ChemInform. 40
Functionalized fused heteroaryl pyrazinones were built up through a novel DBU-catalyzed intramolecular hydroamination reaction of aryl(prop-2-yn-1-yl)-1 H -heteroaryl-2-carboxamides. The nucleophilic addition afforded three isomers; two with an exo -
Autor:
Olaf Kinzel, Edith Monteagudo, Michael Rowley, Sergio Altamura, Odalys Gonzalez Paz, Raffaele De Francesco, Giovanna Pescatore, Philip Jones, Christian Steinkühler, Giuseppe Mesiti, Maria Verdirame
Publikováno v:
Journal of medicinal chemistry. 51(8)
Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin
Autor:
Olaf Kinzel, Laura Llauger-Bufi, Giovanna Pescatore, Michael Rowley, Carsten Schultz-Fademrecht, Edith Monteagudo, Massimiliano Fonsi, Odalys Gonzalez Paz, Fabrizio Fiore, Christian Steinkühler, Philip Jones
Publikováno v:
Journal of Medicinal Chemistry; Jun2009, Vol. 52 Issue 11, p3453-3456, 4p