Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors was written by Zhuang, Rangxiao;Gao, Lixin;Lv, Xiaoqing;Xi, Jianjun;Sheng, Li;Zhao, Yanmei;He, Ruoyu;Hu, Xiaobei;Shao, Yidan;Pan, Xuwang;Liu, Shourong;Huang, Weiwei;Zhou, Yubo;Li, Jia;Zhang, Jiankang. And the article was included in European Journal of Medicinal Chemistry in 2017.SDS of cas: 55661-33-1 This article mentions the following:
A series of novel piperazine or piperidine-containing non-covalent peptidyl derivatives possessing a neopentyl-asparagine residue were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were screened for their 20S proteasome chymotrypsin-like inhibitory activities, and 15 ones displayed more potent activities than carfilzomib with IC50 values lower than 10 nM. Subsequently, the most potent 10 analogs were tested for their cytotoxic activities against two multiple myeloma (MM) cell lines RPMI-8226 and MM-1S. Based on these experiments, selected derivatives were further evaluated for their ex vivo and in vivo blood cell proteasome inhibitory activities. The most potential compound (I) (proteasome inhibition IC50: 1.2 ± 0.1 nM) with potent anti-proliferation (IC50: RPMI-8226 8.4 ± 0.8 nM; MM-1S: 6.3 ± 0.8 nM), ex vivo and in vivo activities also had a prolonged half life in plasma, which demonstrated that the enzymic stabilities of this series of compounds have been improved by constructing a six-membered ring into the peptide skeleton. All the experiments confirmed the correctness of design concept, which made this series of compounds potential leads for exploring new anti-MM drugs. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1SDS of cas: 55661-33-1).
Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.SDS of cas: 55661-33-1
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica