Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.
Publication
, Journal Article
Chamberlain, SD; Wilson, JW; Deanda, F; Patnaik, S; Redman, AM; Yang, B; Shewchuk, L; Sabbatini, P; Leesnitzer, MA; Groy, A; Atkins, C; Lei, H ...
Published in: Bioorg Med Chem Lett
January 15, 2009
The evaluation of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines as inhibitors of the IGF-1R (IGF-IR) receptor tyrosine kinase is reported. Examples demonstrate nanomolar potencies in in vitro enzyme and mechanistic cellular assays as well as promising in vivo pharmacokinetics in rat.
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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
469 / 473
Location
England
Related Subject Headings
- Receptor, IGF Type 1
- Rats
- Pyrimidines
- Protein Kinase Inhibitors
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Drug Discovery
- Animals
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
Citation
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Chicago
ICMJE
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Chamberlain, S. D., Wilson, J. W., Deanda, F., Patnaik, S., Redman, A. M., Yang, B., … Shotwell, J. B. (2009). Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg Med Chem Lett, 19(2), 469–473. https://doi.org/10.1016/j.bmcl.2008.11.046
Chamberlain, Stanley D., Joseph W. Wilson, Felix Deanda, Samarjit Patnaik, Anikó M. Redman, Bin Yang, Lisa Shewchuk, et al. “Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.” Bioorg Med Chem Lett 19, no. 2 (January 15, 2009): 469–73. https://doi.org/10.1016/j.bmcl.2008.11.046.
Chamberlain SD, Wilson JW, Deanda F, Patnaik S, Redman AM, Yang B, et al. Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg Med Chem Lett. 2009 Jan 15;19(2):469–73.
Chamberlain, Stanley D., et al. “Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.” Bioorg Med Chem Lett, vol. 19, no. 2, Jan. 2009, pp. 469–73. Pubmed, doi:10.1016/j.bmcl.2008.11.046.
Chamberlain SD, Wilson JW, Deanda F, Patnaik S, Redman AM, Yang B, Shewchuk L, Sabbatini P, Leesnitzer MA, Groy A, Atkins C, Gerding R, Hassell AM, Lei H, Mook RA, Moorthy G, Rowand JL, Stevens KL, Kumar R, Shotwell JB. Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg Med Chem Lett. 2009 Jan 15;19(2):469–473.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
January 15, 2009
Volume
19
Issue
2
Start / End Page
469 / 473
Location
England
Related Subject Headings
- Receptor, IGF Type 1
- Rats
- Pyrimidines
- Protein Kinase Inhibitors
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Drug Discovery
- Animals
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry