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Newly synthesized curcumin derivatives: crosstalk between chemico-physical properties and biological activity.

Articolo
Data di Pubblicazione:
2011
Citazione:
Newly synthesized curcumin derivatives: crosstalk between chemico-physical properties and biological activity / Ferrari, E., Francesca, P., Imbriano, C., Marverti, G., Valentina, B., Ettore, V., Saladini, M.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 54:(2011), pp. 8066-8077. [10.1021/jm200872q]
Abstract:
New curcumin analogues (ester and acid series) were synthesized with the aim to improve the chemical stability in physiological conditions and potential anticancer activity. Cytotoxicity against different tumorigenic cell lines (human ovarian carcinoma cells – 2008, A2780, C13* and A2780/CP - and human colon carcinoma cells - HCT116 and LoVo) was tested to evaluate cellular specificity and activity.Physico/chemical properties such as acidity, lipophilicity, kinetic stability and free radical scavenging activity were investigated to shed light on the structure-activity relationship and provide new attractive candidates for drug development. Most of ester derivatives show IC50 values lower than curcumin and exhibit selectivity against colon carcinoma cells. Especially they are extremely active after 24h exposure showing enhanced inhibitory effect on cell viability.The best performances of ester curcuminoids could be ascribed to their high lipophilicity that favors a greater and faster cellular uptake overcoming their apparently higher instability in physiological condition.
Tipologia CRIS:
Articolo su rivista
Keywords:
curcumin, synthetic analogues, cytotoxicity, chemico-physical properties, biological activity, ovarian carcinoma, human colon carcinoma
Elenco autori:
Ferrari, Erika; Francesca, Pignedoli; Imbriano, Carol; Marverti, Gaetano; Valentina, Basile; Ettore, Venturi; Saladini, Monica
Autori di Ateneo:
FERRARI Erika
IMBRIANO Carol
MARVERTI Gaetano
Link alla scheda completa:
https://iris.unimore.it/handle/11380/695884
Pubblicato in:
JOURNAL OF MEDICINAL CHEMISTRY
Journal
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URL

http://pubs.acs.org/doi/abs/10.1021/jm200872q
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