Let¡¯s face it, organic chemistry can seem difficult to learn, Formula: C3H3N3O2S, Especially from a beginner¡¯s point of view. Like 121-66-4, Name is 5-Nitrothiazol-2-amine, molecular formula is C8H11Cl2NO2, belongs to pyridine-derivatives compound. In a document, author is Groendyke, Brian J., introducing its new discovery.
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor
Focal adhesion kinase (FAK) is a tyrosine kinase with prominent roles in protein scaffolding, migration, angio-genesis, and anchorage-independent cell survival and is an attractive target for the development of cancer therapeutics. However, current FAK inhibitors display dual kinase inhibition and/or significant activity on several kinases. Although multi-targeted activity is at times therapeutically advantageous, such behavior can also lead to toxicity and confound chemical-biology studies. We report a novel series of small molecules based on a tricyclic pyrimidothiazolodiazepinone core that displays both high potency and selectivity for FAK. Structure-activity relationship (S AR) studies explored modifications to the thiazole, diazepinone, and aniline tail, which identified lead compound BJG-03-025. BJG-03-025 displays potent biochemical FAK inhibition (IC50 = 20 nM), excellent kinome selectivity, activity in 3D-culture breast and gastric cancer models, and favorable pharmacokinetic properties in mice. BJG-03-025 is a valuable chemical probe for evaluation of FAK-dependent biology.
If you are hungry for even more, make sure to check my other article about 121-66-4, Formula: C3H3N3O2S.
Reference:
Thiazole | C3H3NS – PubChem,
,Thiazole | chemical compound | Britannica