Výsledky vyhledávání - "Ester Muraglia"

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists

Autor: Jesus Maria Ontoria Ontoria, Gabriella Dessole, Massimiliano Fonsi, Michael Rowley, Claudio Giuliano, Edith Monteagudo, Christian Steinkühler, Ester Muraglia, Caterina Torrisi, Maria Cecilia Palumbi, Danila Branca, Philip Jones, Laura Llauger Bufi, Alberto Bresciani

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:5283-5288

Smoothened (Smo) antagonists are emerging as new therapies for the treatment of neoplasias with aberrantly reactivated hedgehog (Hh) signaling pathway. A novel series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as smoothened antago

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4799bd47b793aac8f66b445989ccf9c8
https://doi.org/10.1016/j.bmcl.2011.07.030

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Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors

Autor: Federica Orvieto, Danila Branca, Maria Cecilia Palumbi, Philip Jones, Ester Muraglia, Mauro Cerretani, Michael Rowley, Uwe Koch, Carlo Toniatti

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4042-4045

PARP inhibitors have been demonstrated to retard intracellular DNA repair and therefore sensitize tumor cells to cytotoxic agents or ionizing radiation. We report the identification of a novel class of PARP1 inhibitors, containing a pyrrolo moiety fu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20237f15e4288ff8a27f6aabb3450c80
https://doi.org/10.1016/j.bmcl.2009.06.031

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Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors

Autor: Michael Rowley, Isabella Marcucci, Jesus Maria Ontoria Ontoria, Annalise Di Marco, Ester Muraglia, Federica Ferrigno, Christian Steinkühler, Philip Jones, Rita Scarpelli, Ralph Laufer, Sergio Serafini

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:6078-6082

5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based activity. A rapid screening assay

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a5555fb24171b1db1073611f6f6df52
https://doi.org/10.1016/j.bmcl.2008.10.041

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A Functionally Orthogonal Estrogen Receptor-Based Transcription Switch Specifically Induced by a Nonsteroid Synthetic Ligand

Autor: Uwe Koch, Paola Gallinari, Gennaro Ciliberto, Riccardo Cortese, Ester Muraglia, Daniela Fattori, Armin Lahm, Carlo Toniatti, Giuseppe Roscilli, Raffaele De Francesco, Maria Chiara Nardi, Olaf Kinzel, Chantal Paolini

Publikováno v: Chemistry & Biology. 12:883-893

SummaryIt is highly desirable to design ligand-dependent transcription regulation systems based on transactivators unresponsive to endogenous ligands but induced by synthetic small molecules unable to activate endogenous receptors. Using molecular mo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b71375787eca85b43fb384ccb91ce1aa
https://doi.org/10.1016/j.chembiol.2005.05.018

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A novel, inducible, eukaryotic gene expression system based on the quorum‐sensing transcription factor TraR

Autor: Cesare Gargioli, Ester Muraglia, Raffaele De Francesco, Fabio Bonelli, Petra Neddermann, Riccardo Cortese, Sonia Sambucini

Publikováno v: EMBO reports. 4:159-165

Bacteria adapt their pattern of gene expression in response to a variety of external cues, including fluctuations in population density. This type of bacterial cell-to-cell communication is referred to as quorum-sensing. Quorum-sensing systems are pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb9e47bd1c16e601e7eac22cd4e60d31
https://doi.org/10.1038/sj.embor.embor734

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Crystallization and preliminary X-ray diffraction studies of the transcriptional regulator TraR bound to its cofactor and to a specific DNA sequence

Autor: Alessandro Vannini, Raffaele De Francesco, Cesare Gargioli, Petra Neddermann, Cinzia Volpari, Stefania Di Marco, Ester Muraglia

Publikováno v: Acta Crystallographica Section D Biological Crystallography. 58:1362-1364

TraR is an Agrobacterium tumefaciens transcriptional regulator which binds the pheromone N-3-oxooctanoyl-L-homoserine lactone (AAI) in response to the bacterial population density. The TraR-AAI complex dimerizes and interacts with a specific 18-base-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::068613a5885338decd39970c3bd1610a
https://doi.org/10.1107/s0907444902010028

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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

Autor: Samuele Lillini, Carsten Schultz-Fademrecht, Edith Monteagudo, Carlo Toniatti, Ester Muraglia, Olaf Kinzel, Caterina Torrisi, Danila Branca, Laura Llauger Bufi, Federica Ferrigno, Michael Rowley, Philip Jones

Publikováno v: Bioorganicmedicinal chemistry letters. 20(3)

We describe an extensive SAR study in the 6-[4-fluoro-3-(substituted)benzyl]-4,5-dimethylpyridazin-3(2H)-one series which led to the identification of potent PARP-1 inhibitors, capable of inhibiting the proliferation of BRCA-1 deficient cancer cells

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e686ae1c1ebec83055f2a5d980cb77a7
https://pubmed.ncbi.nlm.nih.gov/20022747

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Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)

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-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::182f0fe062b9f1e8432d7af1fa595892
https://pubmed.ncbi.nlm.nih.gov/20031401

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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

Autor: Maria Cecilia Palumbi, Olaf Kinzel, Sergio Serafini, Christian Steinkühler, Michael Rowley, Danila Branca, Gabriella Dessole, Philip Jones, Ester Muraglia, Federica Ferrigno

Publikováno v: Bioorganicmedicinal chemistry letters. 19(15)

We report the synthesis and biological evaluation of N-[(1-aryl-1H-indazol-5-yl)methyl]amide derivatives as Smoothened antagonists and inhibitors of the Hedgehog pathway. Identification of the lead structure 1 by HTS, followed by SAR study on the ami

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::154131357367b4bfede2dd7733afbed4
https://pubmed.ncbi.nlm.nih.gov/19540115

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