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 5000nM, which is a concentration 100 times higher than the parent stilbene 1a.

Design, synthesis and biological evaluation of novel stilbene-based antitumor agents

SIMONI, Daniele;ELEOPRA, Marco;MARCHETTI, Paolo;RONDANIN, Riccardo;BARUCHELLO, Riccardo;GRISOLIA, Giuseppina;
2009

Abstract

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 5000nM, which is a concentration 100 times higher than the parent stilbene 1a.
2009
Simoni, Daniele; Francesco Paolo, Invidiata; Eleopra, Marco; Marchetti, Paolo; Rondanin, Riccardo; Baruchello, Riccardo; Grisolia, Giuseppina; Ashutosh, Tripathi; Glen E., Kellogg; David, Durrant; Ray M., Lee
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/532355
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