On November 1, 2015, Larraufie, Marie-Helene; Yang, Wan Seok; Jiang, Elise; Thomas, Ajit G.; Slusher, Barbara S.; Stockwell, Brent R. published an article.Application In Synthesis of 5-Bromo-2-isopropoxyaniline The title of the article was Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility. And the article contained the following:
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 for compounds to be tested in animal models or in human clin. studies. To overcome this limitation, the authors designed ketone-based functionalities capable of forming reversible covalent adducts, while displaying high metabolic stability, and imparting improved water solubility to their pendant scaffold. The authors tested this strategy on the ferroptosis inducer and exptl. therapeutic erastin, and observed substantial increases in compound potency. In particular, a new carbonyl erastin analog, termed IKE, displayed improved potency, solubility and metabolic stability, thus representing an ideal candidate for future in vivo cancer therapeutic applications. The experimental process involved the reaction of 5-Bromo-2-isopropoxyaniline(cas: 1019442-22-8).Application In Synthesis of 5-Bromo-2-isopropoxyaniline
The Article related to ketone preparation pharmacokinetics, covalent, erastin, ferroptosis, metabolic stability, reactive carbonyl, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 5-Bromo-2-isopropoxyaniline
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary