Bioorganic & medicinal chemistry, 2009-01, Vol.17 (2), p.512-522
2009
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Details
- Autor(en) / Beteiligte
- Titel
- Design, synthesis and biological evaluation of novel stilbene-based antitumor agents
- Ist Teil von
- Bioorganic & medicinal chemistry, 2009-01, Vol.17 (2), p.512-522
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2009
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2008.12.002Titel-ID: cdi_proquest_miscellaneous_66849668
- Format
- –
- Schlagworte
- Amines, Antineoplastic agents, Antineoplastic Agents - chemical synthesis, Antineoplastic Agents - pharmacology, Antitumor agents, Biological and medical sciences, Cell Line, Tumor, Cell Proliferation - drug effects, Dose-Response Relationship, Drug, Drug Design, General aspects, Humans, Medical sciences, Pharmacology. Drug treatments, Prodrugs, Prodrugs - chemistry, Solubility, Stilbenes, Stilbenes - chemical synthesis, Stilbenes - pharmacology, Structure-Activity Relationship, Tubulin - metabolism