Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family was written by Fang, Lincheng;Hu, Zhaoxue;Yang, Yifei;Chen, Pan;Zhou, Jinpei;Zhang, Huibin. And the article was included in Bioorganic & Medicinal Chemistry in 2021.HPLC of Formula: 33050-32-7 This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, 6-Chloro-[1,2,4]triazolo[4,3-b]pyridazin-3(2H)-one (cas: 33050-32-7HPLC of Formula: 33050-32-7).
6-Chloro-[1,2,4]triazolo[4,3-b]pyridazin-3(2H)-one (cas: 33050-32-7) belongs to pyridazine derivatives. Pyridazine-based compounds continued to be a great source of biologically active compounds as evidenced by the number of publications which emerged in 2021. Pyridazine compounds have attracted interest in various fields like medicinal, industrial, and agricultural research as they are used for numerous biological activities and other applications.HPLC of Formula: 33050-32-7
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem