Quality Control of (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HCl《Cancer Selective Target Degradation by Folate-Caged PROTACs》 was published in 2021. The authors were Liu, Jing;Chen, He;Liu, Yi;Shen, Yudao;Meng, Fanye;Kaniskan, H. Umit;Jin, Jian;Wei, Wenyi, and the article was included in《Journal of the American Chemical Society》. The author mentioned the following in the article:
PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin-proteasome system. However, potential toxicity of PROTACs in normal cells due to the off-tissue on-target degradation effect limits their clin. applications. Precise control of a PROTAC’s on-target degradation activity in a tissue-selective manner could minimize potential toxicity/side-effects. To this end, we developed a cancer cell selective delivery strategy for PROTACs by conjugating a folate group to a ligand of the VHL E3 ubiquitin ligase, to achieve targeted degradation of proteins of interest (POIs) in cancer cells vs. noncancerous normal cells. We show that our folate-PROTACs, including BRD PROTAC (folate-ARV-771), MEK PROTAC (folate-MS432), and ALK PROTAC (folate-MS99), are capable of degrading BRDs, MEKs, and ALK, resp., in a folate receptor-dependent manner in cancer cells. This design provides a generalizable platform for PROTACs to achieve selective degradation of POIs in cancer cells. To complete the study, the researchers used (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HCl (cas: 1948273-01-5) .
Quality Control of (S)-1-(4-(4Methylthiazol-5-yl)phenyl)ethan-1-amine HClVarious laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica