Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma was written by Zhang, Wen;Wang, Xueyuan;Zhang, Haoyang;Wen, Tiantian;Yang, Lin;Miao, Hang;Wang, Jia;Liu, Hailong;Yang, Xu;Lei, Meng;Zhu, Yongqiang. And the article was included in Bioorganic & Medicinal Chemistry in 2021.Related Products of 87694-53-9 This article mentions the following:
The ubiquitin proteasome pathway (UPP) plays a critical role in the maintenance of cell homeostasis and the development of diseases, such as cancer and neurodegenerative disease. A series of novel tripeptide propylene oxide compounds as proteasome inhibitors were designed, synthesized and biol. investigated in this manuscript. The enzymic activities of final compounds against 20S human proteasome were investigated and structure-activity relationship (SAR) was summarized. Some potent compounds were further evaluated to inhibit the proliferation of multiple myeloma (MM) cancer cell lines RPMI8226 and U266B. The results showed that some compounds were active against MM cancer cell lines with IC50 values of less than 50 nM. The microsomal metabolic stabilities in human, rat and mice species were carried out and the results showed that compounds (I) (R1 = iso-Bu, Bn) were stable enough to be in vivo investigated. The in vivo pharmacokinetic results showed that compounds I (R1 = iso-Bu, Bn) had acceptable biol. parameters for both ig and iv administrations. In vivo antitumor activities of compounds I (R1 = iso-Bu, Bn) with the doses of 100 mg/kg and 50 mg/kg BIW were performed by using RPMI8226 xenograft nude mouse model. Toxicities of compounds I (R1 = iso-Bu, Bn) were not observed during the experiment and dose dependent effect was obvious and the tumor volume was greatly inhibited. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Related Products of 87694-53-9).
(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Related Products of 87694-53-9
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics