Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Publication
, Journal Article
Chamberlain, SD; Redman, AM; Wilson, JW; Deanda, F; Shotwell, JB; Gerding, R; Lei, H; Yang, B; Stevens, KL; Hassell, AM; Shewchuk, LM; Groy, A ...
Published in: Bioorg Med Chem Lett
January 15, 2009
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.
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
January 15, 2009
Volume
19
Issue
2
Start / End Page
360 / 364
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Receptor, IGF Type 1
- Pyrroles
- Pyrimidines
- Protein Kinase Inhibitors
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- MAP Kinase Kinase 4
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
Citation
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Chamberlain, S. D., Redman, A. M., Wilson, J. W., Deanda, F., Shotwell, J. B., Gerding, R., … Patnaik, S. (2009). Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg Med Chem Lett, 19(2), 360–364. https://doi.org/10.1016/j.bmcl.2008.11.077
Chamberlain, Stanley D., Anikó M. Redman, Joseph W. Wilson, Felix Deanda, J Brad Shotwell, Roseanne Gerding, Huangshu Lei, et al. “Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.” Bioorg Med Chem Lett 19, no. 2 (January 15, 2009): 360–64. https://doi.org/10.1016/j.bmcl.2008.11.077.
Chamberlain SD, Redman AM, Wilson JW, Deanda F, Shotwell JB, Gerding R, et al. Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg Med Chem Lett. 2009 Jan 15;19(2):360–4.
Chamberlain, Stanley D., et al. “Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.” Bioorg Med Chem Lett, vol. 19, no. 2, Jan. 2009, pp. 360–64. Pubmed, doi:10.1016/j.bmcl.2008.11.077.
Chamberlain SD, Redman AM, Wilson JW, Deanda F, Shotwell JB, Gerding R, Lei H, Yang B, Stevens KL, Hassell AM, Shewchuk LM, Leesnitzer MA, Smith JL, Sabbatini P, Atkins C, Groy A, Rowand JL, Kumar R, Mook RA, Moorthy G, Patnaik S. Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg Med Chem Lett. 2009 Jan 15;19(2):360–364.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
January 15, 2009
Volume
19
Issue
2
Start / End Page
360 / 364
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Receptor, IGF Type 1
- Pyrroles
- Pyrimidines
- Protein Kinase Inhibitors
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- MAP Kinase Kinase 4
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry