Fang, Lincheng; Hu, Zhaoxue; Yang, Yifei; Chen, Pan; Zhou, Jinpei; Zhang, Huibin published an article in 2021. The article was titled 《Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family》, and you may find the article in Bioorganic & Medicinal Chemistry.COA of Formula: C4H7NO2S The information in the text is summarized as follows:
Bromodomain and extra-terminal (BET) is a promising therapeutic target for various hematol. cancers. We used the BRD4 inhibitor compound 13 (I) as a lead compound to develop a variety of compounds, and we introduced diverse groups into the position of the compound 13 orienting toward the ZA channel. A series of compounds bearing triazolopyridazine motif exhibited remarkable BRD4 protein inhibitory activities. Among them, compound 39 (II) inhibited BRD4(BD1) protein with an IC50 of 0.003μM which was superior to lead compound 13. Meanwhile, compound 39 possess activity, IC50 = 2.1μM, in antiproliferation activity against U266 cancer cells. On the other hand, compound 39 could arrest tumor cells into the G0/G1 phase and induce apoptosis, which was consistent with its results in inhibiting cell proliferation. Biol. and biochem. data suggest that BRD4 protein might be a therapeutic target and that compound 39 is an excellent lead compound for further development. The experimental process involved the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1COA of Formula: C4H7NO2S)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.COA of Formula: C4H7NO2S
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics