1285539-41-4Relevant academic research and scientific papers
Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site
Du, Yongli,Zhang, Yanhui,Ling, Hao,Li, Qunyi,Shen, Jingkang
, p. 692 - 700 (2018/01/01)
PTP1B serving as a key negative regulator of insulin signaling is a novel target for type 2 diabetes and obesity. Modification at ring B of N-{4-[(3-Phenyl-ureido)-methyl]-phenyl}-methane-sulfonamide template to interact with residues Arg47 and Lys41 in t
The discovery of novel, potent ERR-alpha inverse agonists for the treatment of triple negative breast cancer
Du, Yongli,Song, Lianhua,Zhang, Liudi,Ling, Hao,Zhang, Yanhui,Chen, Haifei,Qi, Huijie,Shi, Xiaojin,Li, Qunyi
, p. 457 - 467 (2017/05/19)
The estrogen-related receptor α (ERRα) is an orphan receptor and a novel target for solid tumor therapy, conceivably through effects on the regulation of tumor cell energy metabolism associated with energy stress within solid tumor micro environments. Here we describe the discovery of novel potent inverse agonists of ERRα. In?vitro, compound 11 potently inhibits ERRα’s transcriptional activity by preventing endogenous PGC-1α and ERRα binding and suppresses the proliferation of different human cancer cell lines and the migration of breast cancer cells (MDA-MB-231). In?vivo, compound 11 demonstrates a strong inhibitory effect on the growth of human breast cancer xenografts (MDA-MB-231) and the tumor growth is inhibited by 40.9% after treating with compound 11 (30?mg/kg). The binding mode shows that compound 11 interacts with the binding pocket of ERRα through hydrogen interactions with the residue Gly397 and hydrophobic interactions with the hydrophobic residues. All these results suggest that compound 11 represents a novel potent ERRα inverse agonist and is promising in the discovery of antitumor compounds for the treatment of triple negative breast cancer.
A 5 - [3 - (2, 5 - diethoxy -4 - mesyl - benzyl) - ureido] -2 - ethoxy - N - phenyl - benzamide new compound, preparation method and use (by machine translation)
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Paragraph 0010, (2017/06/20)
The present invention provides a new compound, the name of the compound is 5 - [3 - (2, 5 - diethoxy -4 - mesyl - benzyl) - ureido] -2 - ethoxy - N - phenyl - benzamide, the molecular weight of this compound 570.6, the structure of the compound (compound 1), see structural formula of; at the same time, the invention provides the compound 1 method for the preparation of; the present invention provides compound has better types of drug resistance, can be used for new drug studies, in particular II type diabetes of innovative pharmaceutical research field. (by machine translation)
Design and Synthesis of Novel Cyclooxygenase-1 Inhibitors as Analgesics: 5-Amino-2-ethoxy-N-(substituted-phenyl)benzamides
Fukai, Ryosuke,Zheng, Xiaoxia,Motoshima, Kazunori,Tai, Akihiro,Yazama, Futoshi,Kakuta, Hiroki
experimental part, p. 550 - 560 (2011/12/22)
We previously found that N-(4-aminophenyl)-4-trifluoromethylbenzamide (TFAP), a COX-1 inhibitor, exhibits an analgesic effect without causing gastric damage. Unfortunately, TFAP causes reddish purple coloration of urine, and its analgesic effect is less potent than that of indomethacin. Herein we describe our study focusing on the development of 4- and 5-amino-2-alkoxy-N-phenylbenzamide scaffolds, designed on the basis of the structures of TFAP and parsalmide, another known COX-1 inhibitory analgesic agent. 5-Amino-2-ethoxy-N-(2- or 3-substituted phenyl)benzamide derivatives exhibited analgesic activity in a murine acetic acid induced writhing test. Among these compounds, 5-amino-2-ethoxy-N-(2-methoxyphenyl)benzamide (9v) possesses potent COX-1 inhibitory and analgesic activities, similar to those of indomethacin. In addition, 5-amino-2-ethoxy-N-(3-trifluoromethylphenyl)benzamide (9g) showed a more potent analgesic effect than indomethacin or 9v without causing apparent gastric damage or coloration of urine, although its COX-1 inhibitory activity was weaker than that of indomethacin or 9v. Thus, 9g and 9v appear to be promising candidates for analgesic agents and are attractive lead compounds for further development of COX-1 inhibitors.
