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Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility

Introducing a reactive carbonyl to a scaffold that does not otherwise have an electrophilic functionality to create a reversible covalent inhibitor is a potentially useful strategy for enhancing compound potency. However, aldehydes are metabolically unstable, which precludes the use of this strategy...

Deskribapen osoa

Gorde:
Xehetasun bibliografikoak
Argitaratua izan da:Bioorg Med Chem Lett
Egile Nagusiak: Larraufie, Marie-Helene, Yang, Wan Seok, Jiang, Elise, Thomas, Ajit G., Slusher, Barbara S., Stockwell, Brent R.
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: 2015
Gaiak:
Sarrera elektronikoa:https://ncbi.nlm.nih.gov/pmc/articles/PMC4653046/
https://ncbi.nlm.nih.gov/pubmed/26231156
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.07.018
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