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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bisi A,Cappadone C,Rampa A,Farruggia G,Sargenti A,Belluti F,Di Martino RMC,Malucelli E,Meluzzi A,Iotti S,Gobbi S

doi

10.1016/j.ejmech.2017.01.020

subject

Has Abstract

pub_date

2017-02-15 00:00:00

pages

577-585

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30028-4

journal_volume

127

pub_type

杂志文章

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