In 2008,Andersen, Carsten B.; Wan, Yongqin; Chang, Jae W.; Riggs, Blake; Lee, Christian; Liu, Yi; Sessa, Fabio; Villa, Fabrizio; Kwiatkowski, Nicholas; Suzuki, Melissa; Nallan, Laxman; Heald, Rebecca; Musacchio, Andrea; Gray, Nathanael S. published 《Discovery of Selective Aminothiazole Aurora Kinase Inhibitors》.ACS Chemical Biology published the findings.Product Details of 3034-22-8 The information in the text is summarized as follows:
Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small mol. aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 Å cocrystal structure with the Aurora B:INCENP complex from Xenopus laevis. The compounds recapitulate the hallmarks of Aurora kinase inhibition, including decreased histone H3 serine 10 phosphorylation, failure to complete cytokinesis, and endoreduplication. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8Product Details of 3034-22-8)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Product Details of 3034-22-8
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica