Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
Тип публикации: Journal Article
Дата публикации: 2011-03-08
scimago Q1
wos Q2
БС1
SJR: 0.805
CiteScore: 5.8
Impact factor: 4
ISSN: 19485875
PubMed ID:
24900315
Organic Chemistry
Drug Discovery
Biochemistry
Краткое описание
The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-Raf(V600E) was developed. Optimization led to the identification of 3-methoxy pyrazolopyridines 17 and 19, potent, selective, and orally bioavailable agents that inhibited tumor growth in a mouse xenograft model driven by B-Raf(V600E) with no effect on body weight. On the basis of their in vivo efficacy and preliminary safety profiles, 17 and 19 were selected for further preclinical evaluation.
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Wenglowsky S. et al. Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors // ACS Medicinal Chemistry Letters. 2011. Vol. 2. No. 5. pp. 342-347.
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Wenglowsky S., Ren L., Ahrendt K. A., Laird E. R., Aliagas I., Alicke B., Buckmelter A. J., F. Choo E., Dinkel V., Feng B., Gloor S., Gould S., Gross S. H., Gunzner Toste J., Hansen J. D., Hatzivassiliou G., Liu B., Malesky K., Simon M., Newhouse B., Raddatz N. J., Ran Y., Rana S., Randolph N., Risom T., Rudolph J., Savage S., Selby L. T., Shrag M., Song K., Sturgis H. L., Voegtli W. C., Wen Z., Willis B. S., Woessner R. D., Wu W., Young W. I., Grina J. Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors // ACS Medicinal Chemistry Letters. 2011. Vol. 2. No. 5. pp. 342-347.
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TY - JOUR
DO - 10.1021/ml200025q
UR - https://doi.org/10.1021/ml200025q
TI - Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
T2 - ACS Medicinal Chemistry Letters
AU - Wenglowsky, Steve
AU - Ren, Li
AU - Ahrendt, Kateri A
AU - Laird, Ellen R
AU - Aliagas, Ignacio
AU - Alicke, Bruno
AU - Buckmelter, Alex J
AU - F. Choo, Edna
AU - Dinkel, Victoria
AU - Feng, Bainian
AU - Gloor, Susan
AU - Gould, Stephen
AU - Gross, Stefan Hubert
AU - Gunzner Toste, Janet
AU - Hansen, Joshua D.
AU - Hatzivassiliou, Georgia
AU - Liu, Bonnie
AU - Malesky, Kim
AU - Simon, Mathieu
AU - Newhouse, Brad
AU - Raddatz, Nicholas J.
AU - Ran, Yingqing
AU - Rana, Sumeet
AU - Randolph, Nikole
AU - Risom, Tyler
AU - Rudolph, Joachim
AU - Savage, Scott
AU - Selby, Leann T
AU - Shrag, Michael
AU - Song, Kyung
AU - Sturgis, Hillary L
AU - Voegtli, Walter C.
AU - Wen, Zhaoyang
AU - Willis, Brandon S
AU - Woessner, Richard D
AU - Wu, Wen-I
AU - Young, Wendy Isobel
AU - Grina, Jonas
PY - 2011
DA - 2011/03/08
PB - American Chemical Society (ACS)
SP - 342-347
IS - 5
VL - 2
PMID - 24900315
SN - 1948-5875
ER -
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@article{2011_Wenglowsky,
author = {Steve Wenglowsky and Li Ren and Kateri A Ahrendt and Ellen R Laird and Ignacio Aliagas and Bruno Alicke and Alex J Buckmelter and Edna F. Choo and Victoria Dinkel and Bainian Feng and Susan Gloor and Stephen Gould and Stefan Hubert Gross and Janet Gunzner Toste and Joshua D. Hansen and Georgia Hatzivassiliou and Bonnie Liu and Kim Malesky and Mathieu Simon and Brad Newhouse and Nicholas J. Raddatz and Yingqing Ran and Sumeet Rana and Nikole Randolph and Tyler Risom and Joachim Rudolph and Scott Savage and Leann T Selby and Michael Shrag and Kyung Song and Hillary L Sturgis and Walter C. Voegtli and Zhaoyang Wen and Brandon S Willis and Richard D Woessner and Wen-I Wu and Wendy Isobel Young and Jonas Grina},
title = {Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors},
journal = {ACS Medicinal Chemistry Letters},
year = {2011},
volume = {2},
publisher = {American Chemical Society (ACS)},
month = {mar},
url = {https://doi.org/10.1021/ml200025q},
number = {5},
pages = {342--347},
doi = {10.1021/ml200025q}
}
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MLA
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Wenglowsky, Steve, et al. “Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.” ACS Medicinal Chemistry Letters, vol. 2, no. 5, Mar. 2011, pp. 342-347. https://doi.org/10.1021/ml200025q.