Chalcones are characterized by possessing an enone moiety between two arom. rings. A series of chalcone-like agents, in which the double bond of the enone system is embedded within a thiophene ring, were synthesized and evaluated for antiproliferative activity and inhibition of tubulin assembly and colchicine binding to tubulin. The replacement of the double bond with a thiophene maintains antiproliferative activity and therefore must not significantly alter the relative conformation of the two aryl rings. The synthesized compds. were found to inhibit the growth of several cancer cell lines at nanomolar to low micromolar concns. In general, all compds. having significant antiproliferative activity inhibited tubulin polymn. with an IC50 < 2 M. Several of these compds. caused K562 cells to arrest in the G2/M phase of the cell cycle.

Design, Synthesis and Biological Evaluation of Thiophene Analogs of Chalcones

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;
2008

Abstract

Chalcones are characterized by possessing an enone moiety between two arom. rings. A series of chalcone-like agents, in which the double bond of the enone system is embedded within a thiophene ring, were synthesized and evaluated for antiproliferative activity and inhibition of tubulin assembly and colchicine binding to tubulin. The replacement of the double bond with a thiophene maintains antiproliferative activity and therefore must not significantly alter the relative conformation of the two aryl rings. The synthesized compds. were found to inhibit the growth of several cancer cell lines at nanomolar to low micromolar concns. In general, all compds. having significant antiproliferative activity inhibited tubulin polymn. with an IC50 < 2 M. Several of these compds. caused K562 cells to arrest in the G2/M phase of the cell cycle.
2008
Romagnoli, Romeo; Baraldi, Pier Giovanni; Taradas S., Carrion M. D.; Lopez Cara, C.; Cruz Lopez, O.; Preti, Delia; Tolomeo, M.; Grimaudo, S.; Di Cristina, A.; Zonta, N.; Balzarini, J.; Brancale, A.; Hamel, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/530091
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