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Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology
[Image: see text] RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key in vivo metabolite of Pz-1 is its less active demethylated pyrazole analogue. Using bioisosteric substitution methods, her...
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| Izdano u: | J Med Chem |
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| Glavni autori: | , , , , , , , , , , , , |
| Format: | Artigo |
| Jezik: | Inglês |
| Izdano: |
American Chemical Society
2020
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| Online pristup: | https://ncbi.nlm.nih.gov/pmc/articles/PMC7901654/ https://ncbi.nlm.nih.gov/pubmed/32298114 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b01336 |
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