Optimisation of a series of indolin-2-one p38α inhibitors was achieved via both blocking of a potential metabolic 'hot spot' and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat. ... In a previous Letter, 2 the design, synthesis and binding mode (as determined by X-ray crystallography) of a series of indolin-2-one based p38α inhibitors, as exemplified by 1 (Fig. 1), was described.
![6-Bromo-2',3',5',6'-tetrahydrospiro[indoline-3,4'-pyran]-2-one Structure](https://image.chemsrc.com/caspic/471/1190861-43-8.png)