《Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Wang, Lei; Jiang, Jingsheng; Zhang, Lixiao; Zhang, Qiuyue; Zhou, Jianrui; Li, Li; Xu, Xiaoli; You, Qidong. Reference of 2-Bromoacetamide The article mentions the following:
Cell division cycle 37 (Cdc37) is known to work as a kinase-specific cochaperone, which selectively regulates the maturation of kinases through protein-protein interaction (PPI) with Hsp90. Directly disrupting the Hsp90-Cdc37 PPI is emerging as an alternative strategy to develop anticancer agents through a specific inhibition manner of kinase clients of Hsp90. Based on a first specific small-mol. inhibitor targeting Hsp90-Cdc37 PPI (DDO-5936), which was previously reported by our group, we conducted a preliminary investigation of the structure-activity relationships and pharmacodynamic evaluations to improve the potency and drug-like properties. Here, our efforts resulted in the currently best inhibitor 18h with improved binding affinity (Kd = 0.5μM) and cellular inhibitory activity (IC50 = 1.73μM). Both in vitro and in vivo assays revealed that 18h could efficiently block the Hsp90-Cdc37 interaction to specifically inhibit kinase clients of Hsp90. Furthermore, 18h showed ideal physiochem. properties with favorable stability, leading to an oral efficacy in vivo. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Reference of 2-Bromoacetamide)
2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Reference of 2-Bromoacetamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics