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PDBsum entry 4d0w
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References listed in PDB file
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Key reference
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Title
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Pyrrole-3-Carboxamides as potent and selective jak2 inhibitors.
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Authors
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M.G.Brasca,
M.Nesi,
N.Avanzi,
D.Ballinari,
T.Bandiera,
J.Bertrand,
S.Bindi,
G.Canevari,
D.Carenzi,
D.Casero,
L.Ceriani,
M.Ciomei,
A.Cirla,
M.Colombo,
S.Cribioli,
C.Cristiani,
F.Della vedova,
G.Fachin,
M.Fasolini,
E.R.Felder,
A.Galvani,
A.Isacchi,
D.Mirizzi,
I.Motto,
A.Panzeri,
E.Pesenti,
P.Vianello,
P.Gnocchi,
D.Donati.
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Ref.
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Bioorg Med Chem Lett, 2014,
22,
4998-5012.
[DOI no: ]
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PubMed id
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Abstract
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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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