Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Publication
, Journal Article
Emmitte, KA; Wilson, BJ; Baum, EW; Emerson, HK; Kuntz, KW; Nailor, KE; Salovich, JM; Smith, SC; Cheung, M; Gerding, RM; Stevens, KL; Mook, RA ...
Published in: Bioorg Med Chem Lett
February 1, 2009
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
February 1, 2009
Volume
19
Issue
3
Start / End Page
1004 / 1008
Location
England
Related Subject Headings
- Receptor, Insulin
- Receptor, IGF Type 1
- Pyridines
- Molecular Conformation
- Models, Chemical
- Mice
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- Drug Design
Citation
APA
Chicago
ICMJE
MLA
NLM
Emmitte, K. A., Wilson, B. J., Baum, E. W., Emerson, H. K., Kuntz, K. W., Nailor, K. E., … Kumar, R. (2009). Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorg Med Chem Lett, 19(3), 1004–1008. https://doi.org/10.1016/j.bmcl.2008.11.058
Emmitte, Kyle A., Brian J. Wilson, Erich W. Baum, Holly K. Emerson, Kevin W. Kuntz, Kristen E. Nailor, James M. Salovich, et al. “Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).” Bioorg Med Chem Lett 19, no. 3 (February 1, 2009): 1004–8. https://doi.org/10.1016/j.bmcl.2008.11.058.
Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, et al. Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004–8.
Emmitte, Kyle A., et al. “Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).” Bioorg Med Chem Lett, vol. 19, no. 3, Feb. 2009, pp. 1004–08. Pubmed, doi:10.1016/j.bmcl.2008.11.058.
Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R. Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004–1008.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
February 1, 2009
Volume
19
Issue
3
Start / End Page
1004 / 1008
Location
England
Related Subject Headings
- Receptor, Insulin
- Receptor, IGF Type 1
- Pyridines
- Molecular Conformation
- Models, Chemical
- Mice
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- Drug Design