Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Publication
, Journal Article
Stellwagen, JC; Adjabeng, GM; Arnone, MR; Dickerson, SH; Han, C; Hornberger, KR; King, AJ; Mook, RA; Petrov, KG; Rheault, TR; Rominger, CM ...
Published in: Bioorg Med Chem Lett
August 1, 2011
A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen.
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
August 1, 2011
Volume
21
Issue
15
Start / End Page
4436 / 4440
Location
England
Related Subject Headings
- Sulfonamides
- Structure-Activity Relationship
- Rats
- Proto-Oncogene Proteins B-raf
- Protein Kinase Inhibitors
- Microsomes, Liver
- Medicinal & Biomolecular Chemistry
- Fluorine
- Catalytic Domain
- Binding Sites
Citation
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Stellwagen, J. C., Adjabeng, G. M., Arnone, M. R., Dickerson, S. H., Han, C., Hornberger, K. R., … Uehling, D. E. (2011). Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg Med Chem Lett, 21(15), 4436–4440. https://doi.org/10.1016/j.bmcl.2011.06.021
Stellwagen, John C., George M. Adjabeng, Marc R. Arnone, Scott H. Dickerson, Chao Han, Keith R. Hornberger, Alastair J. King, et al. “Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.” Bioorg Med Chem Lett 21, no. 15 (August 1, 2011): 4436–40. https://doi.org/10.1016/j.bmcl.2011.06.021.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, et al. Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436–40.
Stellwagen, John C., et al. “Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.” Bioorg Med Chem Lett, vol. 21, no. 15, Aug. 2011, pp. 4436–40. Pubmed, doi:10.1016/j.bmcl.2011.06.021.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE. Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436–4440.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
August 1, 2011
Volume
21
Issue
15
Start / End Page
4436 / 4440
Location
England
Related Subject Headings
- Sulfonamides
- Structure-Activity Relationship
- Rats
- Proto-Oncogene Proteins B-raf
- Protein Kinase Inhibitors
- Microsomes, Liver
- Medicinal & Biomolecular Chemistry
- Fluorine
- Catalytic Domain
- Binding Sites