Synthesis and biological evaluation of diversely substituted indolin-2-ones

Fadoua Bouchikhi (1) , Emilie Rossignol (1) , Martine Sancelme (1) , Bettina Aboab (1) , Fabrice Anizon (1) , Doriano Fabbro (2) , Michelle Prudhomme (1) , Pascale Moreau (1)

1 SEESIB - Synthèse et étude de systèmes à intêret biologique
2 Novartis Pharma AG

The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these compounds toward a panel of eight kinases were examined. Furthermore, the antibacterial activities of the prepared compounds were tested against two Gram-positive bacteria Bacillus cereus and Streptomyces chartreusis, a Gram-negative bacterium Escherichia coli and a yeast Candida albicans.

Domaines: Chimie thérapeutique

Fadoua Bouchikhi, Emilie Rossignol, Martine Sancelme, Bettina Aboab, Fabrice Anizon, et al.. Synthesis and biological evaluation of diversely substituted indolin-2-ones. European Journal of Medicinal Chemistry, 2008, 43, pp.2316-2322. ⟨hal-00333575v1⟩