Electric Literature of C7H5ClN2SOn September 15, 2021 ,《Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing a sulfoxide moiety as anaplastic lymphoma kinase (ALK) inhibition agents》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Wu, Feng; Yao, Han; Li, Wei; Zhang, Niuniu; Fan, Yangyang; Chan, Albert S. C.; Li, Xingshu; An, Baijiao. The article contains the following contents:
Herein, 16 new 2,4-diaminopyrimidines I (R1 = H, F, Cl; R2 = EtS, EtSO, i-PrSO; R3 = Me2NCH2CH2NMe, 4-methylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl, 4-dimethylaminopiperidin-1-yl, etc.; R4 = H, H2N, EtCONH) bearing a sulfide or sulfoxide moiety were synthesized and evaluated for anaplastic lymphoma kinase (ALK) inhibitory activity. The optimal compound I [R1 = F; R2 = EtSO; R3 = 4-methylpiperazin-1-yl; R4 = EtCONH; (II)] exhibited excellent antiproliferative activity against non-small cell lung cancer NCI-H2228 cells, which was better than that of Brigatinib and similar to Ceritinib. Mechanism study revealed that the compound II decreased the mitochondrial membrane potential and arrested NCI-H2228 cells in the G0/G1 phase, finally resulting in cellular apoptosis. It is interesting that the compound II could effectively inhibit the migration of NCI-H2228 cells and may be a promising leading compound for chemotherapy of metastatic cancer. In addition to this study using 6-Chlorobenzothiazol-2-ylamine, there are many other studies that have used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Electric Literature of C7H5ClN2S) was used in this study.
6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Electric Literature of C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica