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PDBsum entry 3nw6
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References listed in PDB file
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Key reference
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Title
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Proline isosteres in a series of 2,4-Disubstituted pyrrolo[1,2-F][1,2,4]triazine inhibitors of igf-1r kinase and ir kinase.
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Authors
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A.J.Sampognaro,
M.D.Wittman,
J.M.Carboni,
C.Chang,
A.F.Greer,
W.W.Hurlburt,
J.S.Sack,
D.M.Vyas.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
5027-5030.
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PubMed id
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Abstract
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Pyrrolidine, pyrrolidinone, carbocyclic, and acyclic groups were used as
isosteric proline replacements in a series of insulin-like growth factor I
receptor kinase/insulin receptor kinase inhibitors. Examples that were similar
in potency to proline-containing reference compounds were shown to project a key
fluoropyridine amide into a common space, while less potent compounds were not
able to do so for reasons of stereochemistry or structural rigidity.
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