Discovery of 2-{4-[(3S)-Piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors
Jones, Philip, Altamura, Sergio, Boueres, Julia, Ferrigno, Federica, Fonsi, Massimiliano, Giomini, Claudia, Lamartina, Stefania, Monteagudo, Edith, Ontoria, Jesus M, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pesci, Silvia, Roscilli, Giuseppe, Scarpelli, Rita, Schultz-Fademrecht, Carsten, Toniatti, Carlo, Rowley, Michael
Published in Journal of medicinal chemistry (26.11.2009)
Published in Journal of medicinal chemistry (26.11.2009)
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Discovery of (7 R )-14-Cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6 H -indolo[1,2- e ][1,5]benzoxazocine-11-carboxylic Acid (MK-3281), a Potent and Orally Bioavailable Finger-Loop Inhibitor of the Hepatitis C Virus NS5B Polymerase
Narjes, Frank, Crescenzi, Benedetta, Ferrara, Marco, Habermann, Jörg, Colarusso, Stefania, del Rosario Rico Ferreira, Maria, Stansfield, Ian, Mackay, Angela Claire, Conte, Immacolata, Ercolani, Caterina, Zaramella, Simone, Palumbi, Maria-Cecilia, Meuleman, Philip, Leroux-Roels, Geert, Giuliano, Claudio, Fiore, Fabrizio, Di Marco, Stefania, Baiocco, Paola, Koch, Uwe, Migliaccio, Giovanni, Altamura, Sergio, Laufer, Ralph, De Francesco, Raffaele, Rowley, Michael
Published in Journal of medicinal chemistry (13.01.2011)
Published in Journal of medicinal chemistry (13.01.2011)
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Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors
Orvieto, Federica, Branca, Danila, Giomini, Claudia, Jones, Philip, Koch, Uwe, Ontoria, Jesus M., Palumbi, Maria Cecilia, Rowley, Michael, Toniatti, Carlo, Muraglia, Ester
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway
Dessole, Gabriella, Branca, Danila, Ferrigno, Federica, Kinzel, Olaf, Muraglia, Ester, Palumbi, Maria Cecilia, Rowley, Michael, Serafini, Sergio, Steinkühler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Journal Article
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2
Kinzel, Olaf, Alfieri, Anna, Altamura, Sergio, Brunetti, Mirko, Bufali, Simone, Colaceci, Fabrizio, Ferrigno, Federica, Filocamo, Gessica, Fonsi, Massimiliano, Gallinari, Paola, Malancona, Savina, Hernando, Jose Ignacio Martin, Monteagudo, Edith, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pucci, Vincenzo, Rowley, Michael, Sasso, Romina, Scarpelli, Rita, Steinkühler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
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Journal Article
N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists
Muraglia, Ester, Ontoria, Jesus M., Branca, Danila, Dessole, Gabriella, Bresciani, Alberto, Fonsi, Massimiliano, Giuliano, Claudio, Llauger Bufi, Laura, Monteagudo, Edith, Palumbi, Maria Cecilia, Torrisi, Caterina, Rowley, Michael, Steinkühler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors
Branca, Danila, Cerretani, Mauro, Jones, Philip, Koch, Uwe, Orvieto, Federica, Palumbi, Maria Cecilia, Rowley, Michael, Toniatti, Carlo, Muraglia, Ester
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Journal Article
Inhibitors of the Hepatitis C Virus NS3 Protease with Basic Amine Functionality at the P3-Amino Acid N-Terminus: Discovery and Optimization of a New Series of P2−P4 Macrocycles
Harper, Steven, Ferrara, Marco, Crescenzi, Benedetta, Pompei, Marco, Palumbi, Maria Cecilia, DiMuzio, Jillian M, Donghi, Monica, Fiore, Fabrizio, Koch, Uwe, Liverton, Nigel J, Pesci, Silvia, Petrocchi, Alessia, Rowley, Michael, Summa, Vincenzo, Gardelli, Cristina
Published in Journal of medicinal chemistry (13.08.2009)
Published in Journal of medicinal chemistry (13.08.2009)
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Development of a Scalable Chiral Synthesis of MK-3281, an Inhibitor of the Hepatitis C Virus NS5B Polymerase
Colarusso, Stefania, Conte, Immacolata, Di Filippo, Marcello, Ercolani, Caterina, Mackay, Angela C., Palumbi, Maria Cecilia, Ferreira, Maria del Rosario Rico, Stansfield, Ian, Zaramella, Simone, Narjes, Frank, Habermann, Joerg
Published in Synlett (01.07.2011)
Published in Synlett (01.07.2011)
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Journal Article
Discovery of (7R)-14-Cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic Acid (MK-3281), a Potent and Orally Bioavailable Finger-Loop Inhibitor of the Hepatitis C Virus NS5B Polymerase
Narjes, Frank, Crescenzi, Benedetta, Ferrara, Marco, Habermann, Jörg, Colarusso, Stefania, del Rosario Rico Ferreira, Maria, Stansfield, Ian, Mackay, Angela Claire, Conte, Immacolata, Ercolani, Caterina, Zaramella, Simone, Palumbi, Maria-Cecilia, Meuleman, Philip, Leroux-Roels, Geert, Giuliano, Claudio, Fiore, Fabrizio, Di Marco, Stefania, Baiocco, Paola, Koch, Uwe, Migliaccio, Giovanni, Altamura, Sergio, Laufer, Ralph, De Francesco, Raffaele, Rowley, Michael
Published in Journal of medicinal chemistry (13.01.2011)
Published in Journal of medicinal chemistry (13.01.2011)
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Journal Article
Identification of Novel, Selective, and Stable Inhibitors of Class II Histone Deacetylases. Validation Studies of the Inhibition of the Enzymatic Activity of HDAC4 by Small Molecules as a Novel Approach for Cancer Therapy
Ontoria, Jesus M, Altamura, Sergio, Di Marco, Annalise, Ferrigno, Federica, Laufer, Ralph, Muraglia, Ester, Palumbi, Maria Cecilia, Rowley, Michael, Scarpelli, Rita, Schultz-Fademrecht, Carsten, Serafini, Sergio, Steinkühler, Christian, Jones, Philip
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Journal Article
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors
MURAGLIA, Ester, ALTAMURA, Sergio, JONES, Philip, BRANCA, Danila, CECCHETTI, Ottavia, FERRIGNO, Federica, ORSALE, Maria Vittoria, PALUMBI, Maria Cecilia, ROWLEY, Michael, SCARPELLI, Rita, STEINKÜHLER, Christian
Published in Bioorganic & medicinal chemistry (01.12.2008)
Published in Bioorganic & medicinal chemistry (01.12.2008)
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Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant
Muraglia, Ester, Kinzel, Olaf D., Laufer, Ralph, Miller, Michael D., Moyer, Gregory, Munshi, Vandna, Orvieto, Federica, Palumbi, Maria Cecilia, Pescatore, Giovanna, Rowley, Michael, Williams, Peter D., Summa, Vincenzo
Published in Bioorganic & medicinal chemistry letters (15.05.2006)
Published in Bioorganic & medicinal chemistry letters (15.05.2006)
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Journal Article
N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxa mide s as highly potent smoothened antagonists
Muraglia, Ester, Ontoria, Jesus M, Branca, Danila, Dessole, Gabriella, Bresciani, Alberto, Fonsi, Massimiliano, Giuliano, Claudio, Bufi, Laura Llauger, Monteagudo, Edith, Palumbi, Maria Cecilia, Torrisi, Caterina, Rowley, Michael, Steinkuehler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
Discovery of 2-{4-[(3 S )-Piperidin-3-yl]phenyl}-2 H -indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors
Jones, Philip, Altamura, Sergio, Boueres, Julia, Ferrigno, Federica, Fonsi, Massimiliano, Giomini, Claudia, Lamartina, Stefania, Monteagudo, Edith, Ontoria, Jesus M., Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pesci, Silvia, Roscilli, Giuseppe, Scarpelli, Rita, Schultz-Fademrecht, Carsten, Toniatti, Carlo, Rowley, Michael
Published in Journal of medicinal chemistry (26.11.2009)
Published in Journal of medicinal chemistry (26.11.2009)
Get full text
Journal Article
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazi n e-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2
Kinzel, Olaf, Alfieri, Anna, Altamura, Sergio, Brunetti, Mirko, Bufali, Simone, Colaceci, Fabrizio, Ferrigno, Federica, Filocamo, Gessica, Fonsi, Massimiliano, Gallinari, Paola, Malancona, Savina, Hernando, Jose Ignacio Martin, Monteagudo, Edith, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pucci, Vincenzo, Rowley, Michael, Sasso, Romina, Scarpelli, Rita, Steinkuehler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
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Journal Article
Identification of MK-5710 ((8 aS)-8 a-methyl-1,3-dioxo-2-[(1 S,2 R)-2-phenylcyclo- propyl]- N-(1-phenyl-1 H-pyrazol-5-yl)hexahydro-imidazo[1,5- a]pyrazine-7(1 H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2
Kinzel, Olaf, Alfieri, Anna, Altamura, Sergio, Brunetti, Mirko, Bufali, Simone, Colaceci, Fabrizio, Ferrigno, Federica, Filocamo, Gessica, Fonsi, Massimiliano, Gallinari, Paola, Malancona, Savina, Hernando, Jose Ignacio Martin, Monteagudo, Edith, Orsale, Maria Vittoria, Palumbi, Maria Cecilia, Pucci, Vincenzo, Rowley, Michael, Sasso, Romina, Scarpelli, Rita, Steinkühler, Christian, Jones, Philip
Published in Bioorganic & medicinal chemistry letters (2011)
Published in Bioorganic & medicinal chemistry letters (2011)
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