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PDBsum entry 3dbf
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References listed in PDB file
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Key reference
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Title
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Design and synthesis of 2-Amino-Pyrazolopyridines as polo-Like kinase 1 inhibitors.
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Authors
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R.V.Fucini,
E.J.Hanan,
M.J.Romanowski,
R.A.Elling,
W.Lew,
K.J.Barr,
J.Zhu,
J.C.Yoburn,
Y.Liu,
B.T.Fahr,
J.Fan,
Y.Lu,
P.Pham,
I.C.Choong,
E.C.Vanderporten,
M.Bui,
H.E.Purkey,
M.J.Evanchik,
W.Yang.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
5648-5652.
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PubMed id
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Abstract
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A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like
kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to
provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the
phenotype of treated cells is consistent with Plk1 inhibition. A co-crystal
structure of one of these compounds with zPlk1 confirms an ATP-competitive
binding mode.
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