Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines

0423094 - ÚEB 2014 RIV FR eng J - Journal Article
Imramovský, A. - Jorda, Radek - Pauk, K. - Řezníčková, Eva - Dušek, J. - Hanousek, J. - Kryštof, Vladimír
Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines.
European Journal of Medicinal Chemistry. Roč. 68, č. 2013 (2013), s. 253-259. ISSN 0223-5234. E-ISSN 1768-3254
R&D Projects: GA ČR GAP305/12/0783; GA ČR GA301/08/1649
Institutional research plan: CEZ:AV0Z50380511
Keywords : Diamides * Apoptosis * Cytotoxicity
Subject RIV: CE - Biochemistry
Impact factor: 3.432, year: 2013

Variously substituted 2-hydroxy-N-(arylallcyl)benzamides were prepared and screened for anti-proliferative and cytotoxic activity in cancer cell lines in vitro. Five compounds, out of 33 showed single-digit micromolar IC50 values against several human cancer cell lines. One of the most potent compounds N-((R)-1-(4-chlorophenylcarbamoyl)-2-phenylethyl)-5-chloro-2-hydroxybenzamide (6k) reduced proliferation and induced apoptosis in the melanoma cell line G361 in a dose-dependent manner, as shown by decrease in 5-bromo-2'-deoxyuridine incorporation and increase in several apoptotic markers, including subdiploid population increase, activation of caspases and site-specific poly-(ADP-ribose)polymerase (PARP) cleavage.
Permanent Link: http://hdl.handle.net/11104/0229347