37536-92-8Relevant articles and documents
Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function
Ye, Zi,Zhang, Xiaoyun,Zhu, Yuangang,Song, Tong,Chen, Xiaowei,Lei, Xiaoguang,Wang, Chu
, p. 2413 - 2422 (2018)
Ethacrynic acid (EA) is a diuretic drug that is widely used to treat high-blood pressure and swelling caused by congestive heart failure or kidney failure. It acts through noncovalent inhibition of the Na+-K+-2Cl- cotransporter in the thick ascending limb of Henle's loop. Chemically, EA contains a Michael acceptor group that can react covalently with nucleophilic residues in proteins; however, the proteome reactivity of EA remains unexplored. Herein, we took a quantitative chemoproteomic approach to globally profile EA's targets in cancer cells. We discovered that EA induces impaired mitochondrial function accompanied by increased ROS production. Our profiling revealed that EA targets functional proteins on mitochondrial membranes, including adenine nucleotide translocases (ANTs). Site-specific mapping identified that EA covalently modifies a functional cysteine in ANTs, a mutation of which resulted in the rescuing effect on EA-induced mitochondrial dysfunction. The newly discovered modes of action offer valuable information to repurpose EA for cancer treatment.
Preparation method of chlorophenoxyacetic ester
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Paragraph 0064; 0066, (2019/01/08)
The invention provides a preparation method of chlorophenoxyacetic ester, wherein the preparation method comprises the following steps: A) carrying out reaction of glycolic acid and alcohol in tolueneto obtain glycolic ester; B) carrying out reaction of glycolic ester and metal alkoxide to obtain a metal salt of glycolic ester; and C) carrying out reaction of the metal salt of glycolic ester andchlorobenzene to obtain the chlorophenoxyacetic ester. The chlorophenoxyacetic ester is synthesized by condensation of chlorobenzene with the metal salt of glycolic ester, the use of chlorophenol withunpleasant odor is effectively avoided, the production of highly toxic dioxins is eliminated, and the product quality and the operating environment of the production site are greatly improved. Motherliquor containing effective ingredients cannot be produced, so the loss of effective ingredients is effectively avoided and the yield of the product is improved.
Synthesis and biological activity of 1-(Substituted phenoxyacetoxy)- 1-(pyridin-2-yl or thien-2-yl)methylphosphonates
Wang, Tao,Wang, Wei,Peng, Hao,He, Hongwu
, p. 173 - 179 (2015/01/30)
A series of novel O,O-dimethyl 1-(substituted phenoxyacetoxy)-1-(pyridin-2-yl or thien-2-yl)methylphosphonates 6a-n and 7a-d were synthesized. Their structures were confirmed by IR, 1H NMR, mass spectroscopy, and elemental analyses. The results of preliminary bioassays show that some of the title compounds exhibit moderate to good herbicidal and fungicidal activities. For example, the title compounds 6a, 6c, 6l, 6m, and 7d possess 90-100% inhibition against most of the tested plants at the dosage of 1500 g ai/ha, whereas the title compounds 6b, 6g-h and 6n possess 92-100% inhibition against Fusarium oxysporum, Phyricularia grisea, Botrytis cinereapers, Gibberella zeae, Sclerotinia sclerotiorum, and Cercospora beticola at the concentration of 50mg/L.