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ID: ALA1165969

Journal: Bioorg Med Chem

Title: Synthesis and cytotoxicity of novel indirubin-5-carboxamides.

Authors: Cheng X, Rasqué P, Vatter S, Merz KH, Eisenbrand G.

Abstract: Indirubins have been reported to act as potent inhibitors of protein kinases relevant to tumorigenesis and of tumor cell growth, but their development to antitumor drugs suffer from their poor water solubility. We synthesized a novel class of indirubin derivatives, indirubin-5-carboxamides, carrying amide substituents with basic centers. Quaternization or protonation of these alkylamino substituents provided indirubins with significantly improved solubility without loss of bioactivity.

CiteXplore: 20488718

DOI: 10.1016/j.bmc.2010.04.066