1334318-75-0Relevant academic research and scientific papers
18-BETA-GLYCYRRHETINIC ACID DERIVATIVES WITH ANTI-TUMOR ACTIVITY
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Page/Page column 57; 58, (2012/03/11)
The invention relates to the medical and cosmetic field, more precisely the field of anticancer treatment and treatment of inflammatory diseases and diabetes and the field of anti-aging or anti-wrinkling agents using newly synthesized 18β-glycyrrhetinic acid derivatives and there use in the treatment of said disorders or symptoms.
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
Lallemand, Benjamin,Chaix, Fabien,Bury, Marina,Bruyère, Céline,Ghostin, Jean,Becker, Jean-Paul,Delporte, Cédric,Gelbcke, Michel,Mathieu, Véronique,Dubois, Jacques,Prévost, Martine,Jabin, Ivan,Kiss, Robert
, p. 6501 - 6513 (2011/11/30)
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 IC50in 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.
