Application of 95-24-9On November 15, 2019 ,《Pyrazolo-benzothiazole hybrids: synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model》 appeared in European Journal of Medicinal Chemistry. The author of the article were Reddy, Velma Ganga; Reddy, T. Srinivasa; Jadala, Chetna; Reddy, M. Soumya; Sultana, Faria; Akunuri, Ravikumar; Bhargava, Suresh K.; Wlodkowic, Donald; Srihari, P.; Kamal, Ahmed. The article conveys some information:
A series of new pyrazolo-benzothiazole hybrids I [R1 = H, MeO, F, Cl; R2 = H, Me, MeO, F, Cl] was synthesized and screened for their anticancer activity against several cancer cell lines [colon (HT-29), prostate (PC-3), lung (A549), glioblastoma (U87MG)] and normal human embryonic kidney cell line (Hek-293T). Compounds I [R1 = H, R2 = F, Cl; R1 = F, R2 = F, Cl; R1 = Cl, R2 = F, Cl; R1 = MeO, R2 = F, Cl] displayed significant anticancer activity against all tested cancer cell lines and compound I [R1 = F, R2 = Cl] showed most potent activity among the series with IC50 values in the range 3.17-6.77 μM, even better than reference drug axitinib (4.88-21.7 μM). Compound I [R1 = F, R2 = Cl] also showed the strongest growth inhibition in 3D multicellular spheroids of PC-3 and U87MG cells. The mechanism of cellular toxicity in PC-3 cells was found to be cell cycle arrest and apoptosis induction through depolarisation of mitochondrial membrane potential, increased ROS production and subsequent DNA damage. Further, compound I [R1 = F, R2 = Cl] displayed significant in vitro (VEGFR-2 inhibition) and in vivo [transgenic zebrafish Tg(flila:EGFP) model] antiangiogenic properties. Overall, these results provided strong evidence that compound I [R1 = F, R2 = Cl] could be considered for a lead candidate in anticancer and antiangiogenic drug discovery. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Application of 95-24-9)
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.Application of 95-24-9Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica