El Abbouchi, Abdelmoula; El Brahmi, Nabil; Hiebel, Marie-Aude; Bignon, Jerome; Guillaumet, Gerald; Suzenet, Franck; El Kazzouli, Said published the artcile< Synthesis and biological evaluation of ethacrynic acid derivatives bearing sulfonamides as potent anti-cancer agents>, Application In Synthesis of 22952-32-5, the main research area is ethacrynic acid sulfonamide preparation anticancer human safety; Anti-cancer; Anti-proliferative; Cancer cells; Ethacrynic acid; Safety ratios; Sulfonamides.
A series of ethacrynic acid (2-[2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetic acid) (EA, Edecrin) containing sulfonamides linked via three types of linkers namely 1,2-ethylenediamine, piperazine and 4-aminopiperidine was synthesized and subsequently evaluated in vitro against HL60 and HCT116 cancer cell lines. All the EA analogs, excluding two derivs, showed anti-proliferative activity with IC50s in the micromolar range (less than 4 uM). Three derivatives I-III were selected for their interesting dual activity on HL60 cell line in order to be further evaluated against a panel of cancer cell lines (HCT116, A549, MCF7, PC3, U87-MG and SKOV3) as well as on MRC5 as a normal cell line. These compounds displayed IC50 values in nanomolar range against A549, MCF7, PC3 and HCT116 cell lines, deducing the discovery that piperazine or 4-aminopiperidine is the linker’s best choice to develop EA analogs with highly potent anti-proliferative activities own up to 24 nM. Besides, in terms of selectivity, those linkers are more suitable offering safety ratios of up to 63.8.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Application In Synthesis of 22952-32-5.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics