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Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. 2009
Daniele Simoni, and
Francesco Paolo Invidiata, and
Marco Eleopra, and
Paolo Marchetti, and
Riccardo Rondanin, and
Riccardo Baruchello, and
Giuseppina Grisolia, and
Ashutosh Tripathi, and
Glen E Kellogg, and
David Durrant, and
Ray M Lee
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, via Fossato di Mortara 17/19, I-44100 Ferrara, Italy. smd@unife.it
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.
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