Výsledky vyhledávání - "Danila Branca"

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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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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Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors

Autor: Philip Jones, Maria Cecilia Palumbi, Michael Rowley, Danila Branca, Claudia Giomini, Uwe Koch, Federica Orvieto, Carlo Toniatti, Jesus Maria Ontoria Ontoria, Ester Muraglia

Publikováno v: Bioorganicmedicinal chemistry letters. 19(15)

A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74901d23a128fdc68b05c418c2fbe1a3
https://pubmed.ncbi.nlm.nih.gov/19541484

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2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors

Autor: Christian Steinkühler, Maria Vittoria Orsale, Michael Rowley, Sergio Altamura, Philip Jones, Danila Branca, Ester Muraglia, Ottavia Cecchetti, Maria Cecilia Palumbi, Rita Scarpelli, Federica Ferrigno

Publikováno v: Bioorganicmedicinal chemistry letters. 18(23)

Trifluoroacetylthiophene carboxamides have recently been reported to be class II HDAC inhibitors, with moderate selectivity. Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f718e2aaa967ba3002bc811a738fa134
https://pubmed.ncbi.nlm.nih.gov/18930398

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