1227476-97-2Relevant academic research and scientific papers
Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines
Imramovsky, Ale?,Jorda, Radek,Pauk, Karel,?ezní?ková, Eva,Du?ek, Jan,Hanusek, Ji?í,Kry?tof, Vladimír
, p. 253 - 259 (2013/10/01)
Variously substituted 2-hydroxy-N-(arylalkyl)benzamides were prepared and screened for antiproliferative 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.
Investigating spectrum of biological activity of 4- and 5-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides
Imramovsky, Ales,Pesko, Matus,Kralova, Katarina,Vejsova, Marcela,Stolarikova, Jirina,Vinsova, Jarmila,Jampilek, Josef
, p. 2414 - 2430 (2011/05/05)
In this study, a series of twenty-two 5-chloro-2-hydroxy-N-[2-(arylamino)- 1- alkyl-2-oxoethyl]benzamides and ten 4-chloro-2-hydroxy-N-[2-(arylamino)-1- alkyl-2- oxoethyl]benzamides is described. The compounds were analyzed using RP-HPLC to determine lipophilicity. Primary in vitro screening of the synthesized compounds was performed against mycobacterial, bacterial and fungal strains. They were also evaluated for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The compounds showed biological activity comparable with or higher than the standards isoniazid, fluconazole, penicillin G or ciprofloxacin. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds as well as their structure-activity relationships are discussed.
