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Michael Rowley

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Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
M Emilia Di Francesco; Fabrizio Fiore; Claudio Giuliano; Edith Monteagudo; Silvia Pesci; Marco Pompei; Vincenzo Pucci; Michael Rowley; Salvatore Avolio; Vincenzo Summa
Synthesis and antiviral properties of novel 7-heterocyclic substituted 7-deaza-adenine nucleoside inhibitors of Hepatitis C NS5B polymerase.

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2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Bioorganic & medicinal chemistry letters 2012;22(23):7207-13.
2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Bioorganic & medicinal chemistry letters 2012;22(23):7201-6.
2012: M Emilia Di Francesco; Fabrizio Fiore; Claudio Giuliano; Edith Monteagudo; Silvia Pesci; Marco Pompei; Vincenzo Pucci; Michael Rowley; Salvatore Avolio; Vincenzo Summa
Synthesis and antiviral properties of novel 7-heterocyclic substituted 7-deaza-adenine nucleoside inhibitors of Hepatitis C NS5B polymerase.
Bioorganic & medicinal chemistry 2012;20(15):4801-11.
2012: Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
Antimicrobial agents and chemotherapy 2012;56(8):4161-7.
2012: M Emilia Di Francesco; Uwe Koch; Marco Pompei; Vincenzo Pucci; Michael Rowley; Salvatore Avolio; Gabriella Dessole; Vincenzo Summa
Synthesis and antiviral properties of novel tetracyclic nucleoside inhibitors of hepatitis C NS5B polymerase.
Nucleosides, nucleotides & nucleic acids 2012;31(8):592-607.
2011: Jesus M Ontoria; Michael Rowley; Sergio Serafini; Christian Steinkühler; Caterina Torrisi; Hu Bin; Alberto Bresciani; Laura Llauger Bufi; Claudia Giomini; Wu Hao; Philip Jones
Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(18):5274-82.
2011: Ester Muraglia; Jesus M Ontoria; Maria Cecilia Palumbi; Michael Rowley; Christian Steinkühler; Caterina Torrisi; Danila Branca; Alberto Bresciani; Gabriella Dessole; Massimiliano Fonsi; Claudio Giuliano; Laura Llauger Bufi; Edith Monteagudo; Philip Jones
N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.
Bioorganic & medicinal chemistry letters 2011;21(18):5283-8.
2011: Savina Malancona; Michael Rowley; Rita Scarpelli; Christian Steinkühler; Sergio Altamura; Gessica Filocamo; Jose Ignacio Martin Hernando; Olaf Kinzel; Philip Jones
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.
Bioorganic & medicinal chemistry letters 2011;21(15):4422-8.
2011: Olaf Kinzel; Savina Malancona; Edith Monteagudo; Maria Orsale; Maria Cecilia Palumbi; Vincenzo Pucci; Michael Rowley; Romina Sasso; Rita Scarpelli; Christian Steinkühler; Anna Alfieri; Sergio Altamura; Mirko Brunetti; Simone Bufali; Fabrizio Colaceci; Federica Ferrigno; Gessica Filocamo; Massimiliano Fonsi; paola gallinari; Jose Ignacio Martin Hernando; Philip Jones
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.
Bioorganic & medicinal chemistry letters 2011;21(15):4429-35.
2011: Bach-Yen T Nguyen; Robin D Isaacs; Hedy Teppler; Randi Y Leavitt; Peter Sklar; Marian Iwamoto; Larissa A Wenning; Michael D Miller; Joshua Chen; Ramon Kemp; Wei Xu; Robert A Fromtling; Joseph P Vacca; Steven D Young; Michael Rowley; Michael W Lower; Keith M Gottesdiener; Daria J Hazuda
Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium.
Annals of the New York Academy of Sciences 2011;1222():83-9.
2011: Frank Narjes; Maria-Cecilia Palumbi; Ian Stansfield; Simone Zaramella; Sergio Altamura; Paola Baiocco; Stefania Colarusso; Immacolata Conte; Benedetta Crescenzi; Raffaele De Francesco; Stefania Di Marco; Caterina Ercolani; Marco Ferrara; Maria del Rosario Rico Ferreira; Fabrizio Fiore; Claudio Giuliano; Jörg Habermann; Uwe Koch; Ralph Laufer; Geert Leroux-Roels; Angela Claire Mackay; Philip Meuleman; Giovanni Migliaccio; Michael Rowley
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.
Journal of medicinal chemistry 2011;54(1):289-301.
2011: Johan Gabrielsson; Ola Fjellström; Johan Ulander; Michael Rowley; Piet H van Der Graaf
Pharmacodynamic-pharmacokinetic integration as a guide to medicinal chemistry.
Current topics in medicinal chemistry 2011;11(4):404-18.
2010: E Monteagudo; M Fonsi; X Chu; K Bleasby; R Evers; V Pucci; Maria Orsale; S Cianetti; M Ferrara; S Harper; R Laufer; Michael Rowley; V Summa
The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease.
Xenobiotica; the fate of foreign compounds in biological systems 2010;40(12):826-39.
2010: Simona Cianetti; Vincent Brett Cooper; Barbara Attenni; Vincenzo Pucci; Fabrizio Fiore; Claudio Giuliano; Ralph Laufer; Cristina Gardelli; Edith Monteagudo; Frank Narjes; Gareth Edward Pearce; Michael Rowley
Enhancement of intestinal absorption of 2-methyl cytidine prodrugs.
Drug delivery 2010;17(4):214-22.
2010: Savina Malancona; Monica Donghi; Marco Ferrara; Josè I Martin Hernando; Marco Pompei; Silvia Pesci; Jesus M Ontoria; Uwe Koch; Michael Rowley; Vincenzo Summa
Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: structure-based design and synthesis of new templates.
Bioorganic & medicinal chemistry 2010;18(8):2836-48.
2010: Giovanna Pescatore; Danila Branca; Fabrizio Fiore; Olaf Kinzel; Laura Llauger Bufi; Ester Muraglia; Federica Orvieto; Michael Rowley; Carlo Toniatti; Caterina Torrisi; Philip Jones
Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Bioorganic & medicinal chemistry letters 2010;20(3):1094-9.
2010: Federica Ferrigno; Danila Branca; Olaf Kinzel; Samuele Lillini; Laura Llauger Bufi; Edith Monteagudo; Ester Muraglia; Michael Rowley; Carsten Schultz-Fademrecht; Carlo Toniatti; Caterina Torrisi; Philip Jones
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Bioorganic & medicinal chemistry letters 2010;20(3):1100-5.
2010: Caterina Torrisi; Monica Bisbocci; Raffaele Ingenito; Jesus M Ontoria; Michael Rowley; Carsten Schultz-Fademrecht; Carlo Toniatti; Philip Jones
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorganic & medicinal chemistry letters 2010;20(2):448-52.
2010: Rita Scarpelli; Julia K Boueres; Mauro Cerretani; Federica Ferrigno; Jesus M Ontoria; Michael Rowley; Carsten Schultz-Fademrecht; Carlo Toniatti; Philip Jones
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(2):488-92.
2009: Philip Jones; Sergio Altamura; Julia Boueres; Federica Ferrigno; Massimiliano Fonsi; Claudia Giomini; Stefania Lamartina; Edith Monteagudo; Jesus M Ontoria; Maria Vittoria Orsale; Maria Cecilia Palumbi; Silvia Pesci; Giuseppe Roscilli; Rita Scarpelli; Carsten Schultz-Fademrecht; Carlo Toniatti; Michael Rowley
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.
Journal of medicinal chemistry 2009;52(22):7170-85.
2009: M Emilia Di Francesco; Gabriella Dessole; Emanuela Nizi; Paola Pace; Uwe Koch; Fabrizio Fiore; Silvia Pesci; Jillian Di Muzio; Edith Monteagudo; Michael Rowley; Vincenzo Summa
Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement.
Journal of medicinal chemistry 2009;52(22):7014-28.
2009: Jesus M Ontoria; Sergio Altamura; Annalise Di Marco; Federica Ferrigno; Ralph Laufer; Ester Muraglia; Maria Cecilia Palumbi; Michael Rowley; Rita Scarpelli; Carsten Schultz-Fademrecht; Sergio Serafini; Christian Steinkühler; Philip Jones
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.
Journal of medicinal chemistry 2009;52(21):6782-9.
2009: Jose Ignacio Martin Hernando; Jesus Maria Ontoria; Savina Malancona; Barbara Attenni; Fabrizio Fiore; Fabio Bonelli; Uwe Koch; Stefania Di Marco; Stefania Colarusso; Simona Ponzi; Nadia Gennari; Sue Ellen Vignetti; Maria Del Rosario Rico Ferreira; Jörg Habermann; Michael Rowley; Frank Narjes
Optimization of thienopyrrole-based finger-loop inhibitors of the hepatitis C virus NS5B polymerase.
ChemMedChem 2009;4(10):1695-713.
2009: M Fonsi; F Fiore; P Jones; O Kinzel; R Laufer; Michael Rowley; E Monteagudo
Metabolism-related liabilities of a potent histone deacetylase (HDAC) inhibitor and relevance of the route of administration on its metabolic fate.
Xenobiotica; the fate of foreign compounds in biological systems 2009;39(10):722-37.
2009: Cristina Gardelli; Barbara Attenni; Monica Donghi; Malte Meppen; Barbara Pacini; Steven Harper; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Vincenzo Pucci; Ralph Laufer; Nadia Gennari; Isabella Marcucci; Joseph F Leone; David B Olsen; Malcolm MacCoss; Michael Rowley; Frank Narjes
Phosphoramidate prodrugs of 2'-C-methylcytidine for therapy of hepatitis C virus infection.
Journal of medicinal chemistry 2009;52(17):5394-407.
2009: Malte Meppen; Barbara Pacini; Renzo Bazzo; Uwe Koch; Joseph F Leone; Kenneth A Koeplinger; Michael Rowley; Sergio Altamura; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Odalys Gonzalez Paz; Ralph Laufer; Vincenzo Pucci; Frank Narjes; Cristina Gardelli
Cyclic phosphoramidates as prodrugs of 2'-C-methylcytidine.
European journal of medicinal chemistry 2009;44(9):3765-70.
2009: Jesus M Ontoria; Edwin H Rydberg; Stefania Di Marco; Licia tomei; Barbara Attenni; Savina Malancona; José I Martin Hernando; Nadia Gennari; Uwe Koch; Frank Narjes; Michael Rowley; Vincenzo Summa; Steve S Carroll; David B Olsen; Raffaele De Francesco; Sergio Altamura; Giovanni Migliaccio; Andrea Carfì
Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.
Journal of medicinal chemistry 2009;52(16):5217-27.
2009: Steven Harper; Marco Ferrara; Benedetta Crescenzi; Marco Pompei; Maria Cecilia Palumbi; Jillian M DiMuzio; Monica Donghi; Fabrizio Fiore; Uwe Koch; Nigel J Liverton; Silvia Pesci; Alessia Petrocchi; Michael Rowley; Vincenzo Summa; Cristina Gardelli
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.
Journal of medicinal chemistry 2009;52(15):4820-37.
2009: Danila Branca; Mauro Cerretani; Philip Jones; Uwe Koch; Federica Orvieto; Maria Cecilia Palumbi; Michael Rowley; Carlo Toniatti; Ester Muraglia
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(15):4042-5.
2009: Federica Orvieto; Danila Branca; Claudia Giomini; Philip Jones; Uwe Koch; Jesus M Ontoria; Maria Cecilia Palumbi; Michael Rowley; Carlo Toniatti; Ester Muraglia
Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(15):4196-200.
2009: Gabriella Dessole; Danila Branca; Federica Ferrigno; Olaf Kinzel; Ester Muraglia; Maria Cecilia Palumbi; Michael Rowley; Sergio Serafini; Christian Steinkühler; Philip Jones
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.
Bioorganic & medicinal chemistry letters 2009;19(15):4191-5.
2009: Alessia Petrocchi; Philip Jones; Michael Rowley; Fabrizio Fiore; Vincenzo Summa
N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(15):4245-9.
2009: 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
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
Journal of medicinal chemistry 2009;52(11):3453-6.
2009: Barbara Attenni; Jesus M Ontoria; Cruz Jonathan; Michael Rowley; Carsten Schultz-Fademrecht; Christian Steinkühler; Philip Jones
Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.
Bioorganic & medicinal chemistry letters 2009;19(11):3081-4.
2009: Ralph Laufer; Odalys Gonzalez Paz; Annalise Di Marco; Fabio Bonelli; Edith Monteagudo; Vincenzo Summa; Michael Rowley
Quantitative prediction of human clearance guiding the development of Raltegravir (MK-0518, isentress) and related HIV integrase inhibitors.
Drug metabolism and disposition: the biological fate of chemicals 2009;37(4):873-83.
2009: Immacolata Conte; Claudio Giuliano; Caterina Ercolani; Frank Narjes; Uwe Koch; Michael Rowley; Sergio Altamura; Raffaele De Francesco; Petra Neddermann; Giovanni Migliaccio; Ian Stansfield
Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture.
Bioorganic & medicinal chemistry letters 2009;19(6):1779-83.
2009: Monica Donghi; Barbara Attenni; Cristina Gardelli; Annalise Di Marco; Fabrizio Fiore; Claudio Giuliano; Ralph Laufer; Joseph F Leone; Vincenzo Pucci; Michael Rowley; Frank Narjes
Synthesis and evaluation of novel phosphoramidate prodrugs of 2'-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2009;19(5):1392-5.
2009: Ian Stansfield; Caterina Ercolani; Angela Mackay; Immacolata Conte; Marco Pompei; Uwe Koch; Nadia Gennari; Claudio Giuliano; Michael Rowley; Frank Narjes
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.
Bioorganic & medicinal chemistry letters 2009;19(3):627-32.
2008: Rita Scarpelli; Annalise Di Marco; Federica Ferrigno; Ralph Laufer; Isabella Marcucci; Ester Muraglia; Jesus M Ontoria; Michael Rowley; Sergio Serafini; Christian Steinkühler; Philip Jones
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(23):6078-82.
2008: Ester Muraglia; Sergio Altamura; Danila Branca; Ottavia Cecchetti; Federica Ferrigno; Maria Orsale; Maria Cecilia Palumbi; Michael Rowley; Rita Scarpelli; Christian Steinkühler; Philip Jones
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(23):6083-7.
2008: Giovanna Pescatore; Olaf Kinzel; Barbara Attenni; Ottavia Cecchetti; Fabrizio Fiore; Massimiliano Fonsi; Michael Rowley; Carsten Schultz-Fademrecht; Sergio Serafini; Christian Steinkühler; Philip Jones
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(20):5528-32.
2008: Vincenzo Summa; Alessia Petrocchi; Fabio Bonelli; Benedetta Crescenzi; Monica Donghi; Marco Ferrara; Fabrizio Fiore; Cristina Gardelli; Odalys Gonzalez Paz; Daria J Hazuda; Philip Jones; Olaf Kinzel; Ralph Laufer; Edith Monteagudo; Ester Muraglia; Emanuela Nizi; Federica Orvieto; Paola Pace; Giovanna Pescatore; Rita Scarpelli; Kara A Stillmock; Marc V Witmer; Michael Rowley
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Journal of medicinal chemistry 2008;51(18):5843-55.
2008: Paola Pace; Michael Rowley
Integrase inhibitors for the treatment of HIV infection.
Current opinion in drug discovery & development 2008;11(4):471-9.
2008: Philip Jones; Matthew J Bottomley; Andrea Carfí; Ottavia Cecchetti; Federica Ferrigno; Paola Lo Surdo; Jesus M Ontoria; Michael Rowley; Rita Scarpelli; Carsten Schultz-Fademrecht; Christian Steinkühler
2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(11):3456-61.
2008: Philip Jones; Sergio Altamura; Raffaele De Francesco; Odalys Gonzalez Paz; Olaf Kinzel; Giuseppe Mesiti; Edith Monteagudo; Giovanna Pescatore; Michael Rowley; Maria Verdirame; Christian Steinkühler
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
Journal of medicinal chemistry 2008;51(8):2350-3.
2008: M Emilia Di Francesco; Paola Pace; Fabrizio Fiore; Francesca Naimo; Fabio Bonelli; Michael Rowley; Vincenzo Summa
Development of 2-t butyl-N-methyl pyrimidones as potent inhibitors of HIV integrase.
Bioorganic & medicinal chemistry letters 2008;18(8):2709-13.
2008: Philip Jones; Sergio Altamura; Raffaele De Francesco; paola gallinari; Armin Lahm; Petra Neddermann; Michael Rowley; Sergio Serafini; Christian Steinkühler
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
Bioorganic & medicinal chemistry letters 2008;18(6):1814-9.
2008: Ester Muraglia; Olaf Kinzel; Cristina Gardelli; Benedetta Crescenzi; Monica Donghi; Marco Ferrara; Emanuela Nizi; Federica Orvieto; Giovanna Pescatore; Ralph Laufer; Odalys Gonzalez Paz; Annalise Di Marco; Fabrizio Fiore; Edith Monteagudo; Massimiliano Fonsi; Peter J Felock; Michael Rowley; Vincenzo Summa
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Journal of medicinal chemistry 2008;51(4):861-74.
2008: Michael Rowley
The discovery of raltegravir, an integrase inhibitor for the treatment of HIV infection.
Progress in medicinal chemistry 2008;46():1-28.
2007: Cristina Gardelli; Emanuela Nizi; Ester Muraglia; Benedetta Crescenzi; Marco Ferrara; Federica Orvieto; Paola Pace; Giovanna Pescatore; Marco Poma; Maria Del Rosario Rico Ferreira; Rita Scarpelli; Carl F Homnick; Norihiro Ikemoto; Anna Alfieri; Maria Verdirame; Fabio Bonelli; Odalys Gonzalez Paz; Marina Taliani; Edith Monteagudo; Silvia Pesci; Ralph Laufer; Peter J Felock; Kara A Stillmock; Daria J Hazuda; Michael Rowley; Vincenzo Summa
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Journal of medicinal chemistry 2007;50(20):4953-75.
2007: Ian Stansfield; Marco Pompei; Immacolata Conte; Caterina Ercolani; Giovanni Migliaccio; Mark Jairaj; Claudio Giuliano; Michael Rowley; Frank Narjes
Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2007;17(18):5143-9.
2007: Edith Monteagudo; Silvia Pesci; Marina Taliani; F Fiore; Alessia Petrocchi; Emanuela Nizi; Michael Rowley; Ralph Laufer; Vincenzo Summa
Studies of metabolism and disposition of potent human immunodeficiency virus (HIV) integrase inhibitors using 19F-NMR spectroscopy.
Xenobiotica; the fate of foreign compounds in biological systems 2007;37(9):1000-12.
2007: Paola Pace; M Emilia Di Francesco; Cristina Gardelli; Steven Harper; Ester Muraglia; Emanuela Nizi; Federica Orvieto; Alessia Petrocchi; Marco Poma; Michael Rowley; Rita Scarpelli; Ralph Laufer; Odalys Gonzalez Paz; Edith Monteagudo; Fabio Bonelli; Daria J Hazuda; Kara A Stillmock; Vincenzo Summa
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
Journal of medicinal chemistry 2007;50(9):2225-39.
2006: Philip Jones; Sergio Altamura; Prasun K Chakravarty; Ottavia Cecchetti; Raffaele De Francesco; paola gallinari; Raffaele Ingenito; Peter T Meinke; Alessia Petrocchi; Michael Rowley; Rita Scarpelli; Sergio Serafini; Christian Steinkühler
A series of novel, potent, and selective histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(23):5948-52.
2006: Vincenzo Summa; Alessia Petrocchi; Victor G Matassa; Cristina Gardelli; Ester Muraglia; Michael Rowley; Odalys Gonzalez Paz; Ralph Laufer; Edith Monteagudo; Paola Pace
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
Journal of medicinal chemistry 2006;49(23):6646-9.
2006: Jesus M Ontoria; Jose I Martìn Hernando; Savina Malancona; Barbara Attenni; Ian Stansfield; Immacolata Conte; Caterina Ercolani; Jörg Habermann; Simona Ponzi; Marcello Di Filippo; Uwe Koch; Michael Rowley; Frank Narjes
Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase.
Bioorganic & medicinal chemistry letters 2006;16(15):4026-30.
2006: Ester Muraglia; Olaf Kinzel; Ralph Laufer; Michael D Miller; Gregory Moyer; Vandna Munshi; Federica Orvieto; Maria Cecilia Palumbi; Giovanna Pescatore; Michael Rowley; Peter D Williams; Vincenzo Summa
Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.
Bioorganic & medicinal chemistry letters 2006;16(10):2748-52.
2005: Claudio Giuliano; F Fiore; Annalise Di Marco; J Padron Velazquez; A Bishop; Fabio Bonelli; Odalys Gonzalez Paz; Isabella Marcucci; Steven Harper; Frank Narjes; Barbara Pacini; Edith Monteagudo; Giovanni Migliaccio; Michael Rowley; Ralph Laufer
Preclinical pharmacokinetics and metabolism of a potent non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Xenobiotica; the fate of foreign compounds in biological systems 2005;35(10-11):1035-54.
2005: Stefania Di Marco; Cinzia Volpari; Licia tomei; Sergio Altamura; Steven Harper; Frank Narjes; Uwe Koch; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio; Andrea Carfí
Interdomain communication in hepatitis C virus polymerase abolished by small molecule inhibitors bound to a novel allosteric site.
The Journal of biological chemistry 2005;280(33):29765-70.
2005: Steven Harper; Salvatore Avolio; Barbara Pacini; Marcello Di Filippo; Sergio Altamura; Licia tomei; Giacomo Paonessa; Stefania Di Marco; Andrea Carfi; Claudio Giuliano; Julio Padron; Fabio Bonelli; Giovanni Migliaccio; Raffaele De Francesco; Ralph Laufer; Michael Rowley; Frank Narjes
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.
Journal of medicinal chemistry 2005;48(14):4547-57.
2005: Steven Harper; Barbara Pacini; Salvatore Avolio; Marcello Di Filippo; Giovanni Migliaccio; Ralph Laufer; Raffaele De Francesco; Michael Rowley; Frank Narjes
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
Journal of medicinal chemistry 2005;48(5):1314-7.
2004: James Crawforth; John R Atack; Susan M Cook; Karl R Gibson; Alan Nadin; Andrew P Owens; Andrew Pike; Michael Rowley; Alison J Smith; Bindi Sohal; Francine Sternfeld; Keith A Wafford; Leslie J Street
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
Bioorganic & medicinal chemistry letters 2004;14(7):1679-82.
2003: Licia tomei; Sergio Altamura; Linda Bartholomew; Antonino Biroccio; Alessandra Ceccacci; Laura Pacini; Frank Narjes; Nadia Gennari; Monica Bisbocci; Ilario Incitti; Laura Orsatti; Steven Harper; Ian Stansfield; Michael Rowley; Raffaele De Francesco; Giovanni Migliaccio
Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Journal of virology 2003;77(24):13225-31.
2002: Karl R Gibson; Laure Hitzel; Russell Mortishire-Smith; Ute Gerhard; Richard A Jelley; Austin J Reeve; Michael Rowley; Alan Nadin; Andrew P Owens
Synthesis and conformational dynamics of tricyclic pyridones containing a fused seven-membered ring.
The Journal of organic chemistry 2002;67(26):9354-60.
2002: Ian Collins; Christopher Moyes; William B Davey; Michael Rowley; Frances A Bromidge; Kathleen Quirk; John R Atack; Ruth M McKernan; Sally-Anne Thompson; Keith A Wafford; Gerard R Dawson; Andrew Pike; Bindi Sohal; Nancy N Tsou; Richard G Ball; José L Castro
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Journal of medicinal chemistry 2002;45(9):1887-900.
2001: Michael Rowley; David J Hallett; Simon C Goodacre; Christopher Moyes; James Crawforth; T J Sparey; S Patel; Rose Marwood; Smita Patel; Steven Thomas; Laure Hitzel; desmond oconnor; Nicola Szeto; José L Castro; Peter H Hutson; Angus M MacLeod
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Journal of medicinal chemistry 2001;44(10):1603-14.
2001: Michael Rowley; Linda J Bristow; Peter H Hutson
Current and novel approaches to the drug treatment of schizophrenia.
Journal of medicinal chemistry 2001;44(4):477-501.
2000: James Crawforth; Simon C Goodacre; R Maxey; S Bourrain; Smita Patel; Rose Marwood; desmond oconnor; R Herbert; Peter H Hutson; Michael Rowley
3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Bioorganic & medicinal chemistry letters 2000;10(24):2701-3.
2000: Ian Collins; William B Davey; Michael Rowley; Kathleen Quirk; Frances A Bromidge; Ruth M McKernan; Sally-Anne Thompson; Keith A Wafford
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
Bioorganic & medicinal chemistry letters 2000;10(12):1381-4.
1999: Monique B van Niel; Ian Collins; Margaret S Beer; Howard B Broughton; Susan K F Cheng; Simon C Goodacre; A Heald; Karen Locker; Angus M MacLeod; Denise Morrison; Christopher Moyes; desmond oconnor; Andrew Pike; Michael Rowley; Michael G N Russell; Bindi Sohal; Josephine A Stanton; Steven Thomas; H Verrier; Alan P Watt; José L Castro
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Journal of medicinal chemistry 1999;42(12):2087-104.
1999: Kevin W Moore; K Bonner; E A Jones; F Emms; Paul D Leeson; Rose Marwood; Smita Patel; S Patel; Michael Rowley; Steven Thomas; Robert W Carling
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Bioorganic & medicinal chemistry letters 1999;9(9):1285-90.
1998: S Bourrain; Ian Collins; Joseph G Neduvelil; Michael Rowley; Paul D Leeson; Smita Patel; S Patel; F Emms; Rose Marwood; Kerry L Chapman; AE Fletcher; GA Showell
Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor.
Bioorganic & medicinal chemistry 1998;6(10):1731-43.
1998: Ian Collins; Michael Rowley; William B Davey; F Emms; Rose Marwood; Smita Patel; S Patel; A Fletcher; I C Ragan; Paul D Leeson; A L Scott; TP Broten
3-(1-piperazinyl)-4,5-dihydro-1H-benzo[g]indazoles: high affinity ligands for the human dopamine D4 receptor with improved selectivity over ion channels.
Bioorganic & medicinal chemistry 1998;6(6):743-53.
1997: Michael Rowley; Janusz J Kulagowski; Alan P Watt; D Rathbone; GI Stevenson; Robert W Carling; R Baker; George R Marshall; J A Kemp; A C Foster; Sarah Grimwood; Richard Hargreaves; C Hurley; KL Saywell; mark david tricklebank; Paul D Leeson
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
Journal of medicinal chemistry 1997;40(25):4053-68.
1997: Michael Rowley; Ian Collins; Howard B Broughton; William B Davey; R Baker; F Emms; Rose Marwood; Smita Patel; S Patel; C Ian Ragan; SB Freedman; R Ball; Paul D Leeson
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Journal of medicinal chemistry 1997;40(15):2374-85.
1996: Michael Rowley; Howard B Broughton; Ian Collins; R Baker; F Emms; Rose Marwood; Smita Patel; S Patel; C Ian Ragan; S B Freedman; Paul D Leeson
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Journal of medicinal chemistry 1996;39(10):1943-5.
1995: Sarah Grimwood; Janusz J Kulagowski; I M Mawer; Michael Rowley; Paul D Leeson; A C Foster
Allosteric modulation of the glutamate site on the NMDA receptor by four novel glycine site antagonists.
European journal of pharmacology 1995;290(3):221-6.
1994: mark david tricklebank; Linda J Bristow; Peter H Hutson; Paul D Leeson; Michael Rowley; KL Saywell; L Singh; F David Tattersall; L Thorn; B J Williams
The anticonvulsant and behavioural profile of L-687,414, a partial agonist acting at the glycine modulatory site on the N-methyl-D-aspartate (NMDA) receptor complex.
British journal of pharmacology 1994;113(3):729-36.
1994: Janusz J Kulagowski; R Baker; Neil R Curtis; Paul D Leeson; I M Mawer; A M Moseley; Mark P Ridgill; Michael Rowley; I Stansfield; A C Foster
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
Journal of medicinal chemistry 1994;37(10):1402-5.
1993: Michael Rowley; Paul D Leeson; GI Stevenson; A M Moseley; I Stansfield; I Sanderson; L Robinson; R Baker; J A Kemp; George R Marshall
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex.
Journal of medicinal chemistry 1993;36(22):3386-96.