911282-07-0Relevant articles and documents
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 2 - butoxypolyethylene -5 - [3 - (2, 5 - diethoxy -4 - mesyl - benzyl) - ureido] - benzoic acid methyl ester the new compound, preparation method and use (by machine translation)
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, (2017/04/11)
The present invention provides a new compound, the names of the compounds 2 - butoxypolyethylene -5 - [3 - (2, 5 - diethoxy -4 - mesyl - benzyl) - ureido] - benzoic acid methyl ester, the molecular weight of this compound 537.6, the structure of the compo
Hydrogen-bonding-mediated anthranilamide homoduplexes. Increasing stability through preorganization and iterative arrangement of a simple amide binding site
Zhu, Jiang,Lin, Jian-Bin,Xu, Yun-Xiang,Shao, Xue-Bin,Jiang, Xi-Kui,Li, Zhan-Ting
, p. 12307 - 12313 (2007/10/03)
This paper describes the assembly of two new series of self-complementary duplexes by making use of amide units, the simplest assembling units of hydrogen bonding, as binding sites. All the new monomers possess a rigidified anthranilamide skeleton, which is stabilized by intramolecular hydrogen bonding. Amide units are iteratively introduced to one side of the preorganized skeletons to facilitate the formation of intermolecular hydrogen bonding. Compounds 2 and 3 bear two and three CONH2 units, respectively, while 4, 6, and 7 are incorporated with two, three, and four AcNH units, respectively. For comparison, compound 5, which is similar to 4 but contains one AcNH and one CF3CONH unit, is also prepared. X-ray diffraction analysis of 2, 4, and 5 revealed homodimeric motifs in the solid state which are stabilized by two or more intermolecular hydrogen bonds. 1H NMR investigations in CDCl3 indicated that all the compounds form hydrogen-bonded homoduplexes. Duplexes 3-3, 6-6, and 7-7 are highly stable in CDCl3, with a lower Kassoc limit of 2.3 × 10 5 M-1. The Kassoc values of the three duplexes in more polar CDCl3/CD3CN (9:1, v/v) were determined with the 1H NMR dilution method. The result opens the way for the development of new polymeric duplexes of well-ordered structures.
