Li, Qifei et al. published their research in Bioorganic & Medicinal Chemistry in 2020 | CAS: 16312-21-3

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine derivatives have been found to exhibit very prominent anti-inflammatory and anti-nociceptive activity. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Synthetic Route of C4H5NO2S

Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors was written by Li, Qifei;Li, Jieming;Cai, Yan;Zou, Yuxing;Chen, Bin;Zou, Feng;Mo, Jiaxian;Han, Ting;Guo, Weiwei;Huang, Wenlong;Qiu, Qianqian;Qian, Hai. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Synthetic Route of C4H5NO2S This article mentions the following:

Bromodomain-containing protein 4 (BRD4) is a key epigenetic regulator in cancer; and inhibitors targeting BRD4 exhibit great anticancer activity. By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors I (R = OEt, OH, tert-butylamino, cyclopropylamino, piperidin-1-yl, morpholin-4-yl, etc.) and II were designed and synthesized. Compound I [R = cyclopentylamino] (III) had a hydrophobic acetylcyclopentanyl side chain, showing the most potent BRD4 inhibitory activity in the BRD4-BD1 inhibition assay (IC50 value of 110 nM), and it also significantly suppressed the proliferation of MV-4-11 cells with high BRD4 level (IC50 value of 0.42μM). Furthermore, the potent apoptosis-promoting and G0/G1 cycle-arresting activities of compound III were indicated by flow cytometry. As the downstream-protein of BRD4, c-Myc was in significantly low expression by compound III treatment in a dose-dependent manner. All the findings supported that the novel compound III provided a perspective for developing effective BRD4 inhibitors. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Synthetic Route of C4H5NO2S).

3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidine derivatives have been found to exhibit very prominent anti-inflammatory and anti-nociceptive activity. Thiazolidines are also used in peptide and protein modification, protein chemical synthesis, as activators to innate immunity and also act as immunostimulating agents.Synthetic Route of C4H5NO2S

Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com