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Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors. 2014
Maria Gabriella Brasca, and
Marcella Nesi, and
Nilla Avanzi, and
Dario Ballinari, and
Tiziano Bandiera, and
Jay Bertrand, and
Simona Bindi, and
Giulia Canevari, and
Davide Carenzi, and
Daniele Casero, and
Lucio Ceriani, and
Marina Ciomei, and
Alessandra Cirla, and
Maristella Colombo, and
Sabrina Cribioli, and
Cinzia Cristiani, and
Franco Della Vedova, and
Gabriele Fachin, and
Marina Fasolini, and
Eduard R Felder, and
Arturo Galvani, and
Antonella Isacchi, and
Danilo Mirizzi, and
Ilaria Motto, and
Achille Panzeri, and
Enrico Pesenti, and
Paola Vianello, and
Paola Gnocchi, and
Daniele Donati
Nerviano Medical Sciences S.r.l., Oncology, Viale Pasteur 10, 20014 Nerviano (MI), Italy. Electronic address: gabriella.brasca@nervianoms.com.
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). Compound 28 displayed significant tumour growth inhibition in SET-2 xenograft tumour model, with a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favourable pharmacokinetic and safety profile.
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Jay Bertrand, and
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Davide Carenzi, and
Daniele Casero, and
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Marina Ciomei, and
Alessandra Cirla, and
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Sabrina Cribioli, and
Cinzia Cristiani, and
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Gabriele Fachin, and
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Davide Carenzi, and
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Maristella Colombo, and
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Antonella Isacchi, and
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Nilla Avanzi, and
Dario Ballinari, and
Tiziano Bandiera, and
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Simona Bindi, and
Giulia Canevari, and
Davide Carenzi, and
Daniele Casero, and
Lucio Ceriani, and
Marina Ciomei, and
Alessandra Cirla, and
Maristella Colombo, and
Sabrina Cribioli, and
Cinzia Cristiani, and
Franco Della Vedova, and
Gabriele Fachin, and
Marina Fasolini, and
Eduard R Felder, and
Arturo Galvani, and
Antonella Isacchi, and
Danilo Mirizzi, and
Ilaria Motto, and
Achille Panzeri, and
Enrico Pesenti, and
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Paola Gnocchi, and
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Simona Bindi, and
Giulia Canevari, and
Davide Carenzi, and
Daniele Casero, and
Lucio Ceriani, and
Marina Ciomei, and
Alessandra Cirla, and
Maristella Colombo, and
Sabrina Cribioli, and
Cinzia Cristiani, and
Franco Della Vedova, and
Gabriele Fachin, and
Marina Fasolini, and
Eduard R Felder, and
Arturo Galvani, and
Antonella Isacchi, and
Danilo Mirizzi, and
Ilaria Motto, and
Achille Panzeri, and
Enrico Pesenti, and
Paola Vianello, and
Paola Gnocchi, and
Daniele Donati
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Marcella Nesi, and
Nilla Avanzi, and
Dario Ballinari, and
Tiziano Bandiera, and
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Simona Bindi, and
Giulia Canevari, and
Davide Carenzi, and
Daniele Casero, and
Lucio Ceriani, and
Marina Ciomei, and
Alessandra Cirla, and
Maristella Colombo, and
Sabrina Cribioli, and
Cinzia Cristiani, and
Franco Della Vedova, and
Gabriele Fachin, and
Marina Fasolini, and
Eduard R Felder, and
Arturo Galvani, and
Antonella Isacchi, and
Danilo Mirizzi, and
Ilaria Motto, and
Achille Panzeri, and
Enrico Pesenti, and
Paola Vianello, and
Paola Gnocchi, and
Daniele Donati
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