A small library of coumarins, carrying butynyl-amino chains, was synthesized continuing our studies in the field of MDR reverting ageEnts and in order to obtain multipotent agents to combat malignancies. In particular, the reported anticancer and chemopreventive natural product 7-isopentenyloxycoumarin was linked to different terminal amines, selected on the basis of our previously reported results. The anticancer behaviour and the MDR reverting ability of the new compounds were evaluated on human colon cancer cells, particularly prone to develop the MDR phenotype. Some of the new derivatives showed promising effects, directly acting as cytotoxic compounds and/or counteracting MDR phenomenon. Compound 1e emerged as the most interesting of this series, showing a multipotent biological profile and suggesting that conjugation of an appropriate coumarin core with a properly selected butynyl-amino chain allows to obtain novel hybrid molecules endowed with improved in vitro antitumor activity.

Alessandra Bisi, Concettina Cappadone, Rampa Angela, Farruggia Giovanna, Sargenti Azzurra, Belluti Federica, et al. (2017). Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 127, 577-585 [10.1016/j.ejmech.2017.01.020].

Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity

BISI, ALESSANDRA;CAPPADONE, CONCETTINA;RAMPA, ANGELA;FARRUGGIA, GIOVANNA;SARGENTI, AZZURRA;BELLUTI, FEDERICA;MALUCELLI, EMIL;IOTTI, STEFANO;GOBBI, SILVIA
2017

Abstract

A small library of coumarins, carrying butynyl-amino chains, was synthesized continuing our studies in the field of MDR reverting ageEnts and in order to obtain multipotent agents to combat malignancies. In particular, the reported anticancer and chemopreventive natural product 7-isopentenyloxycoumarin was linked to different terminal amines, selected on the basis of our previously reported results. The anticancer behaviour and the MDR reverting ability of the new compounds were evaluated on human colon cancer cells, particularly prone to develop the MDR phenotype. Some of the new derivatives showed promising effects, directly acting as cytotoxic compounds and/or counteracting MDR phenomenon. Compound 1e emerged as the most interesting of this series, showing a multipotent biological profile and suggesting that conjugation of an appropriate coumarin core with a properly selected butynyl-amino chain allows to obtain novel hybrid molecules endowed with improved in vitro antitumor activity.
2017
Alessandra Bisi, Concettina Cappadone, Rampa Angela, Farruggia Giovanna, Sargenti Azzurra, Belluti Federica, et al. (2017). Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 127, 577-585 [10.1016/j.ejmech.2017.01.020].
Alessandra Bisi; Concettina Cappadone; Rampa Angela; Farruggia Giovanna; Sargenti Azzurra; Belluti Federica; Rita M.C. Di Martino; Malucelli, Emil; M...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/586436
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