Upadhyay, Neha;Tilekar, Kalpana;Safuan, Sabreena;Kumar, Alan P.;Schweipert, Markus;Meyer-Almes, Franz-Josef;Ramaa, Cs published 《Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2》 in 2021. The article was appeared in 《Future Medicinal Chemistry》. They have made some progress in their research.Category: thiazole The article mentions the following:
Angiogenesis deregulation is often linked to cancer and is thus an essential target. Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. B1, PB11 and PB16 showed HUVEC′s IC50 scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity. The experimental procedure involved many compounds, such as 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .
6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Category: thiazole) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica