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N-(2-{3-[3,5-bis(trifluoromethyl)phenyl]ureido}ethyl)-glycyrrhetinamide (6b): a novel anticancer glycyrrhetinic acid derivative that targets the proteasome and displays anti-kinase activity.

Abstract：

:18-β-Glycyrrhetinic acid (GA; 1) and many of its derivatives are cytotoxic in cancer cells. The current study aims to characterize the anticancer effects of 17 novel 1 derivatives. On the basis of these studies, N-(2-{3-[3,5-bis(trifluoromethyl)phenyl]ureido}ethyl)-glycyrrhetinamide (6b) appeared to be the most potent compound, with IC(50)in vitro growth inhibitory concentrations in single-digit micromolarity in a panel of 8 cancer cell lines. Compound 6b is cytostatic and displays similar efficiency in apoptosis-sensitive versus apoptosis-resistant cancer cell lines through, at least partly, the inhibition of the activity of a cluster of a dozen kinases that are implicated in cancer cell proliferation and in the control of the actin cytoskeleton organization. Compound 6b also inhibits the activity of the 3 proteolytic units of the proteasome. Compound 6b thus represents an interesting hit from which future compounds could be derived to improve chemotherapeutic regimens that aim to combat cancers associated with poor prognoses.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Lallemand B,Chaix F,Bury M,Bruyère C,Ghostin J,Becker JP,Delporte C,Gelbcke M,Mathieu V,Dubois J,Prévost M,Jabin I,Kiss R

doi

10.1021/jm200285z

subject

Has Abstract

pub_date

2011-10-13 00:00:00

pages

6501-13

issue

19

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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