Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Maria Gabriella Brasca"'
Autor:
Marina Ciomei, Ciro Mercurio, Enrico Pesenti, Jurgen Moll, Antonella Isacchi, Arturo Galvani, Francesco Colotta, Fulvia Roletto, Veronica Patton, Wilma Pastori, Giuseppe Locatelli, Francesco Fiorentini, Claudio Festuccia, Maria Gabriella Brasca, Dario Ballinari, Nilla Avanzi, Nadia Amboldi, Rachele Alzani, Clara Albanese
Altered expression and activity of cyclin-dependent kinase (CDK) and tropomyosin receptor kinase (TRK) families are observed in a wide variety of tumors. In those malignancies with aberrant CDK activation, the retinoblastoma protein (pRb) pathway is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4bb653415d9936d93679b97e43a99b1
https://doi.org/10.1158/1535-7163.c.6532245.v1
https://doi.org/10.1158/1535-7163.c.6532245.v1
Autor:
Achille Panzeri, G. Canevari, Sabrina Cribioli, Nadia Amboldi, Nilla Avanzi, Paola Gnocchi, Jay Bertrand, Arturo Galvani, Marina Ciomei, Simona Bindi, Eduard R. Felder, Gabriele Fachin, Ilaria Motto, Antonella Isacchi, Daniele Casero, Daniele Donati, Nicoletta Colombo, Maria Gabriella Brasca, Marcella Nesi
Publikováno v:
Bioorganic & Medicinal Chemistry. 23:2387-2407
Compound 1, a hit from the screening of our chemical collection displaying activity against JAK2, was deconstructed for SAR analysis into three regions, which were explored. A series of compounds was synthesized leading to the identification of the p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c6a5bcbfb3e197406e730be2c53f92e
https://doi.org/10.1016/j.bmc.2015.03.059
https://doi.org/10.1016/j.bmc.2015.03.059
Autor:
Laura Riceputi, Eduard R. Felder, Francesco Sola, Claudio Dalvit, Elena Casale, Arturo Galvani, Carlo Visco, Nadia Amboldi, Francesco Casuscelli, Antonella Isacchi, Gianpaolo Fogliatto, Paolo Polucci, Nicoletta Colombo, Fabio Zuccotto, Maria Gabriella Brasca, Dannica Caronni
Publikováno v:
Bioorganic & Medicinal Chemistry. 22:4135-4150
In the last decade the heat shock protein 90 (Hsp90) has emerged as a major therapeutic target and many efforts have been dedicated to the discovery of Hsp90 inhibitors as new potent anticancer agents. Here we report the identification of a novel cla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b98e9ca68874dbb0db4f02380c73746
https://doi.org/10.1016/j.bmc.2014.05.056
https://doi.org/10.1016/j.bmc.2014.05.056
Autor:
Jay Bertrand, Dario Ballinari, Paolo Cappella, Michele Caruso, Francesco Fiorentini, Alessandra Scolaro, Italo Beria, Laura Gianellini, Barbara Valsasina, Marina Caldarelli, Maria Gabriella Brasca
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:96-101
The discovery and characterization of two new chemical classes of potent and selective Polo-like kinase 1 (PLK1) inhibitors is reported. For the most interesting compounds, we discuss the biological activities, crystal structures and preliminary phar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::912628e99927a261c288c2a65d023ede
https://doi.org/10.1016/j.bmcl.2011.11.065
https://doi.org/10.1016/j.bmcl.2011.11.065
Autor:
Roberto Bossi, Daniele Pezzetta, Gabriele Fachin, Barbara Forte, Alessandra Scolaro, Italo Beria, Walter Ceccarelli, Enrico Pesenti, Michele Caruso, Francesco Fiorentini, Stefania Re Depaolini, Marina Fasolini, Helena Posteri, Barbara Valsasina, Maria Gabriella Brasca
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2969-2974
As part of our drug discovery effort, we identified and developed 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. We now report the optimization of this class that led to the identification of NMS-P937, a potent, selective a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb1c72f2e8179a8a325d3bbb4369e24
https://doi.org/10.1016/j.bmcl.2011.03.054
https://doi.org/10.1016/j.bmcl.2011.03.054
Autor:
Arturo Galvani, Ciro Mercurio, Enrico Pesenti, Jean-Charles Soria, Vladimir Lazar, Thierry de Baere, Matteo Bertolotti, Antonella Isacchi, Francesco Fiorentini, Angela Scaburri, Raffaele A. Calogero, Roberta Bosotti, Emanuela Scacheri, Maria Gabriella Brasca, Giuseppe Locatelli, Marina Ciomei
Publikováno v:
Molecular Cancer Therapeutics. 9:1265-1273
A transcriptional signature of the pan–cyclin-dependent kinase (Cdk) inhibitor PHA-793887 was evaluated as a potential pharmacodynamic and/or response biomarker in tumor and skin biopsies from patients treated in a phase I clinical study. We first
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e2e5f9ab4186763e82fdf50cc1fbcf6
https://doi.org/10.1158/1535-7163.mct-09-1163
https://doi.org/10.1158/1535-7163.mct-09-1163
Autor:
Nilla Avanzi, Wilma Pastori, Marina Ciomei, Valter Croci, James R. Bischoff, Elena Casale, Francesco Fiorentini, Maria Gabriella Brasca, Ciro Mercurio, Paolo Pevarello, Clara Albanese, Rachele Alzani, Antonella Isacchi, Anna Vulpetti, Mario Varasi, Paolo Orsini, Daniela Borghi, Enrico Pesenti, Patrick Roussel, Dario Ballinari, Raffaella Amici, Marcella Nesi, Daniele Volpi
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:1844-1853
We have recently reported CDK inhibitors based on the 6-substituted pyrrolo[3,4-c]pyrazole core structure. Improvement of inhibitory potency against multiple CDKs, antiproliferative activity against cancer cell lines and optimization of the physico-c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9e3228318332fc37ba03b9ea13c1ff4
https://doi.org/10.1016/j.bmc.2010.01.042
https://doi.org/10.1016/j.bmc.2010.01.042
Autor:
J.A. Bertrand, Paolo Pevarello, Patrizia Crivori, Anna Vulpetti, Alexander D. Cameron, Maria Gabriella Brasca, Roberto D'Alessio
Publikováno v:
Journal of Chemical Information and Modeling. 45:1282-1290
An evaluation and comparison of two different approaches, GRID/CPCA and GRIND/CPCA (CPCA = consensus principal component analysis; GRIND = GRid-INdependent Descriptors), suitable for visualizing the structural differences between related proteins is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9374a5fcbc168bff566c5d8b09eb2b0e
https://doi.org/10.1021/ci0500280
https://doi.org/10.1021/ci0500280
Autor:
Nilla Avanzi, Sabrina Cribioli, Paola Gnocchi, Jay Bertrand, Danilo Mirizzi, Daniele Casero, Arturo Galvani, Paola Vianello, Maristella Colombo, Eduard R. Felder, Gabriele Fachin, Achille Panzeri, Lucio Ceriani, G. Canevari, Franco Della Vedova, Dario Ballinari, Cinzia Cristiani, Enrico Pesenti, Marcella Nesi, Tiziano Bandiera, Marina Ciomei, Alessandra Cirla, Maria Gabriella Brasca, Antonella Isacchi, Daniele Donati, Ilaria Motto, Simona Bindi, Marina Fasolini, Davide Carenzi
Publikováno v:
Bioorganicmedicinal chemistry. 22(17)
We report herein the discovery, structure guided design, synthesis and biological evaluation of a novel class of JAK2 inhibitors. Optimization of the series led to the identification of the potent and orally bioavailable JAK2 inhibitor 28 (NMS-P953).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc0c075da4c4b914848e8b7a2755d219
https://pubmed.ncbi.nlm.nih.gov/25009002
https://pubmed.ncbi.nlm.nih.gov/25009002
Publikováno v:
Tetrahedron Letters. 38:4881-4884
α,α-Bis(trifluoromethylbenzyl)triflates offer a convenient access to the corresponding amines through SN1 type reactions.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c41c10c6ab7835622c5e28d900ce038d
https://doi.org/10.1016/s0040-4039(97)01018-6
https://doi.org/10.1016/s0040-4039(97)01018-6