In 2006,Vulpetti, Anna; Casale, Elena; Roletto, Fulvia; Amici, Raffaella; Villa, Manuela; Pevarello, Paolo published 《Structure-based drug design to the discovery of new 2-aminothiazole CDK2 inhibitors》.Journal of Molecular Graphics & Modelling published the findings.SDS of cas: 3034-22-8 The information in the text is summarized as follows:
N-(5-Bromo-1,3-thiazol-2-yl)butanamide (compound 1) was found active (IC50 = 808 nM) in a high throughput screening (HTS) for CDK2 inhibitors. By exploiting crystal structures of several complexes between CDK2 and inhibitors and applying structure-based drug design (SBDD), we rapidly discovered a very potent and selective CDK2 inhibitor 4-[(5-isopropyl-1,3-thiazol-2-yl)amino] benzenesulfonamide (compound 4, IC50 = 20 nM). The syntheses, structure-based analog design, kinases inhibition data and x-ray crystallog. structures of CDK2/inhibitor complexes are reported. The results came from multiple reactions, including the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8SDS of cas: 3034-22-8)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.SDS of cas: 3034-22-8
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica