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PDBsum entry 4c62
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References listed in PDB file
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Key reference
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Title
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Discovery of 1-Methyl-1h-Imidazole derivatives as potent jak2 inhibitors.
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Authors
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Q.Su,
S.Ioannidis,
C.Chuaqui,
L.Almeida,
M.Alimzhanov,
G.Bebernitz,
K.Bell,
M.Block,
T.Howard,
S.Huang,
D.Huszar,
J.A.Read,
C.Rivard costa,
J.Shi,
M.Su,
M.Ye,
M.Zinda.
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Ref.
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J Med Chem, 2014,
57,
144-158.
[DOI no: ]
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PubMed id
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Abstract
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Structure based design, synthesis, and biological evaluation of a novel series
of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT
pathway, are described. Using the C-ring fragment from our first clinical
candidate AZD1480 (24), optimization of the series led to the discovery of
compound 19a, a potent, orally bioavailable Jak2 inhibitor. Compound 19a
displayed a high level of cellular activity in hematopoietic cell lines
harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound 19a
demonstrated significant tumor growth inhibition in a UKE-1 xenograft model
within a well-tolerated dose range.
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Secondary reference #1
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Title
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Discovery of 5-Chloro-N2-[(1s)-1-(5-Fluoropyrimidin-2-Yl)ethyl]-N4-(5-Methyl-1h-Pyrazol-3-Yl)pyrimidine-2,4-Diamine (azd1480) as a novel inhibitor of the jak/stat pathway.
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Authors
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S.Ioannidis,
M.L.Lamb,
T.Wang,
L.Almeida,
M.H.Block,
A.M.Davies,
B.Peng,
M.Su,
H.J.Zhang,
E.Hoffmann,
C.Rivard,
I.Green,
T.Howard,
H.Pollard,
J.Read,
M.Alimzhanov,
G.Bebernitz,
K.Bell,
M.Ye,
D.Huszar,
M.Zinda.
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Ref.
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J Med Chem, 2011,
54,
262-276.
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PubMed id
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