Musdal, Yaman;Hegazy, Usama M.;Aksoy, Yasemin;Mannervik, Bengt published 《FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1》 in 2013. The article was appeared in 《Chemico-Biological Interactions》. They have made some progress in their research.Electric Literature of C14H21Br2ClN2 The article mentions the following:
Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compounds used for other indications would be a shortcut to clin. applications and a search for GST P1-1 inhibitors among approved drugs and other compounds was therefore conducted. We tested 1040 FDA-approved compounds as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC50 values in the low micromolar range. For comparison, these compounds were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione saturation of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compounds investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants. The experimental procedure involved many compounds, such as 2,4-Dibromo-6-((cyclohexyl(methyl)amino)methyl)aniline hydrochloride (cas: 611-75-6) .
2,4-Dibromo-6-((cyclohexyl(methyl)amino)methyl)aniline hydrochloride(cas: 611-75-6) is a mucolytic agent that exerts both a secretagogic action on submucosal glands and a mucolytic action toward acid glycoproteins inside cells. Bromhexine Hydrochloride is a medication prescribed for coughs which works by dissolving hard phlegm. OthersBromhexine is a mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. In addition, bromhexine has antioxidant properties. Electric Literature of C14H21Br2ClN2
Reference:
Bromide – Wikipedia,
bromide – Wiktionary