Water‐Soluble Cationic Derivatives of Indirubin,the Active Anticancer Component from Indigo naturalis |
| |
| Authors: | Werner Ginzinger Alexander Egger Gerhard Mühlgassner Vladimir B. Arion Michael A. Jakupec Markus Galanski Walter Berger Bernhard K. Keppler |
| |
| Affiliation: | 1. University of Vienna, Institute of Inorganic Chemistry, W?hringer Str. 42, A‐1090?Vienna, (phone: +43?1427752600;2. fax: +43?1427752680);3. Research Platform ‘Translational Cancer Therapy Research', Vienna;4. Medical University of Vienna, Institute of Cancer Research, Borschkeg. 8a, A‐1090 Vienna |
| |
| Abstract: | To overcome the problem of poor aqueous solubility and bioavailability of indirubin‐3‐oximes, the compounds were modified by attaching a quaternary ammonium group at the oxime moiety. Exploring the prodrug concept, an oxime ester with acetyl‐l‐ carnitine was prepared, and the rate of its hydrolysis was investigated to assess its suitability for clinical administration. In addition, the cytotoxic potency of new stable oxime ethers with a choline moiety and their influence on the cell cycle were tested in human cancer cell lines. |
| |
| Keywords: | Indirubin L‐Carnitine, acetyl‐ Oxime ester Choline Oxime ether Cytotoxic activity |
|
|
