In 2016,Koblan, Luke W.; Buckley, Dennis L.; Ott, Christopher J.; Fitzgerald, Mark E.; Ember, Stuart W. J.; Zhu, Jin-Yi; Liu, Shuai; Roberts, Justin M.; Remillard, David; Vittori, Sarah; Zhang, Wei; Schonbrunn, Ernst; Bradner, James E. published 《Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET》.ChemMedChem published the findings.Synthetic Route of C10H22N2O2 The information in the text is summarized as follows:
Evaluating the engagement of a small mol. ligand with a protein target in cells provides useful information for chem. probe optimization and pharmaceutical development. While several techniques exist that can be performed in a low-throughput manner, systematic evaluation of large compound libraries remains a challenge. In-cell engagement measurements are especially useful when evaluating compound classes suspected to target multiple cellular factors. In this study we used a bioluminescent resonant energy transfer assay to assess bromodomain engagement by a compound series containing bromodomain- and kinase-biasing polypharmacophores based on the known dual BRD4 bromodomain/PLK1 kinase inhibitor BI2536. With this assay, we discovered several novel agents with bromodomain-selective specificity profiles and cellular activity. Thus, this platform aids in distinguishing mols. whose cellular activity is difficult to assess due to polypharmacol. effects. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Synthetic Route of C10H22N2O2)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Synthetic Route of C10H22N2O2
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