期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 13, 页码 7347-7354出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00508
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资金
- CAPES/INCT-INOFAR [88887.3182253/2019-00]
- DAAD [5749963]
- Baden-Wurttembergisches Brasilien-Zentrum from the University of Tubingen
- Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) under Germany's Excellence Strategy [EXC 2180-390900677]
- Federal Ministry of Education and Research (BMBF)
- Baden-Wurttemberg Ministry of Science as part of the Excellence Strategy of the German Federal Government
- Baden-Wurttemberg Ministry of Science as part of the Excellence Strategy of the German State Government
- Orion Research Foundation
- European Union's Horizon 2020 research and innovation programme under the Marie Sklodowska-Curie [839230]
- German cancer network DKTK
- Frankfurt Cancer Centre (FCI)
- SGC, a registered charity
- AbbVie
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genome Canada
- Innovative Medicines Initiative (EU/EFPIA)
- Janssen
- Merck KGaA Darmstadt Germany
- MSD
- Novartis Pharma AG
- Ontario Ministry of Economic Development and Innovation
- Pfizer
- Sao Paulo Research Foundation-FAPESP
- Takeda
- Wellcome Trust
- Marie Curie Actions (MSCA) [839230] Funding Source: Marie Curie Actions (MSCA)
The recent disclosure of type I 1/2 inhibitors for p38 alpha MAPK demonstrated how the stabilization of the R-spine can be used as a strategy to greatly increase the target residence time (TRT) of inhibitors. Herein, for the first time, we describe N-acylhydrazone and selenophene residues as spine motifs, yielding metabolically stable inhibitors with high potency on enzymatic, NanoBRET, and whole blood assays, improved metabolic stability, and prolonged TRT.
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