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Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 2009 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 19, pages 360-364 (issn: 0960-894X,

Authors: Kirk L. Stevens; Felix Deanda; Samarjit Patnaik; Anikó M. Redman; Rakesh Kumar; Robert A. Mook; Arthur Groy; +14 Authors

doi: 10.1016/j.bmcl.2008.11.077

pmid: 19071018

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

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Abstract

The SAR of C5' functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.

Related Organizations

Research Triangle Park Foundation
United States
Cellzome, GSK, Middlesex, UK.
GlaxoSmithKline (United States)
United States

Keywords

Models, Molecular, Structure-Activity Relationship, Pyrimidines, MAP Kinase Kinase 4, Pyrroles, Protein Kinase Inhibitors, Receptor, IGF Type 1

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BindingDB Entry 3083: Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity
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Mitogen-activated protein kinase 8
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Insulin receptor
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Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

7 Research products, page 1 of 1

3ELJ

3ELJ

BindingDB Entry 3083: Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity

Mitogen-activated protein kinase 8

Insulin receptor

3EKN

3EKN