Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Laura Llauger"'
Autor:
Laura Llauger Bufi, Caterina Torrisi, Christian Steinkühler, Philip Jones, Claudia Giomini, Wu Hao, Sergio Serafini, Alberto Bresciani, Jesus Maria Ontoria Ontoria, Hu Bin, Michael Rowley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5274-5282
The Hedgehog (Hh-) signalling pathway is a key developmental pathway and there is a growing body of evidence showing that this pathway is aberrantly reactivated in a number of human tumors. Novel agents capable of inhibiting this pathway are sought,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3760eb32a5ddf670cd4ed2882c960c7
https://doi.org/10.1016/j.bmcl.2011.07.031
https://doi.org/10.1016/j.bmcl.2011.07.031
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
https://doi.org/10.1016/j.bmcl.2011.07.030
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdcfe67490c8eaffda7f94edfef89fdb
https://doi.org/10.1021/jm9004303
https://doi.org/10.1021/jm9004303
Autor:
Laura Llauger, Julia Aguirre, Nian Wu, Gabriela Chiosis, Joungnam Kim, Huazhong He, R.M. Immormino, Danuta Zatorska, Daniel T. Gewirth, Yuhong She
Publikováno v:
Journal of Medicinal Chemistry. 49:381-390
Hsp90 is a chaperone protein that allows cancer cells to tolerate the many components of dysregulated pathways. Its inactivation may result in targeting multiple molecular alterations and, thus, in reverting the transformed phenotype. The PU-class, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::932f12110b7887f26efc72261834d560
https://doi.org/10.1021/jm0508078
https://doi.org/10.1021/jm0508078
Autor:
Gabriela Chiosis, Neal Rosen, Julia Aguirre, Joungnam Kim, Peter Davies, Laura Llauger, Huazhong He, Ulf Peters
Publikováno v:
Journal of Medicinal Chemistry. 48:2892-2905
Hsp90 is a chaperone protein with important roles in maintaining transformation and in elevating the survival and growth potential of cancer cells. Currently there is an increasing interest in developing inhibitors of this protein as anticancer thera
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f379005d9e88499ef98de22ce18c688
https://doi.org/10.1021/jm049012b
https://doi.org/10.1021/jm049012b
Publikováno v:
Tetrahedron Letters. 40:3961-3964
The addition of a series of stabilized carbon nucleophiles to 3-acyl-1-alkylpyridinium salts. followed by acylation of the intermediate dihydropyridines with trichloroacetic anhydride has been studied. The C-4 adducts resulting from the addition of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::404b0c8bef2163ab8df1fdda43b6046e
https://doi.org/10.1016/s0040-4039(99)00621-8
https://doi.org/10.1016/s0040-4039(99)00621-8
Publikováno v:
Organic Letters. 4:3083-3085
[reaction: see text] Efficient photodecarboxylation of (3-benzoylphenyl)alkanoic acids with formation of carbanions has enabled the determination of their protonation rate constants in water; the values obtained show that the reactivity toward proton
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f341094b56f7a5b7e298d72428d99d8
https://doi.org/10.1021/ol0263752
https://doi.org/10.1021/ol0263752
Publikováno v:
ChemInform. 30
The addition of a series of stabilized carbon nucleophiles to 3-acyl-1-alkylpyridinium salts. followed by acylation of the intermediate dihydropyridines with trichloroacetic anhydride has been studied. The C-4 adducts resulting from the addition of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::67a0182b7968f82f906b8607f237e18d
https://doi.org/10.1002/chin.199935155
https://doi.org/10.1002/chin.199935155
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
https://pubmed.ncbi.nlm.nih.gov/20022747
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
https://pubmed.ncbi.nlm.nih.gov/20031401