Synthesis and cytotoxicity of novel indirubin-5-carboxamides
Xinlai Cheng1, Paul Rasqué, Sandra Vatter
1Department of Chemistry, Division of Food Chemistry and Toxicology, University of Kaiserslautern, Kaiserslautern, Germany.
Bioorganic & Medicinal Chemistry
|May 22, 2010
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.
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