Characterization of Covalent-Reversible EGFR Inhibitors was written by Smith, Steven;Keul, Marina;Engel, Julian;Basu, Debjit;Eppmann, Simone;Rauh, Daniel. And the article was included in ACS Omega in 2017.Formula: C13H17BN2O2 This article mentions the following:
Within the spectrum of kinase inhibitors, covalent-reversible inhibitors (CRIs) provide a valuable alternative approach to classical covalent inhibitors. This special class of inhibitors can be optimized for an extended drug-target residence time. For CRIs, it was shown that the fast addition of thiols to electron-deficient olefins leads to a covalent bond that can break reversibly under proteolytic conditions. Research groups are just beginning to include CRIs in their arsenal of compound classes, and, with that, the understanding of this interesting set of chem. warheads is growing. However, systems to assess both characteristics of the covalent-reversible bond in a simple exptl. setting are sparse. Here, we have developed an efficient methodol. to characterize the covalent and reversible properties of CRIs and to investigate their potential in targeting clin. relevant variants of the receptor tyrosine kinase EGFR. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Formula: C13H17BN2O2).
7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Formula: C13H17BN2O2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles