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A series of novel stilbene derivatives has been synthesized and studied with the main goal to investigate SAR of the amino compound
1a, as well as to improve its water solubility, a potentially negative aspect of the molecule that could be a serious obstacle for a pre-clinical development. We have obtained derivatives with good cytotoxic activity, in particular, the derivatives
5c and
6b could represent two novel leads for further investigation. Compound
8b, a morpholino-carbamate derivative, prodrug of
1a, has a very good solubility in water, and is active in suppressing growth of tumor cells at a concentration of 5000
nM, which is a concentration 100 times higher than the parent stilbene
1a.