370-50-3Relevant articles and documents
COMPOUND HAVING PROTEIN TYROSINE PHOSPHATASE SHP-1 AGONIST ACTIVITY
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Paragraph 0111; 0117, (2018/07/29)
A compound having a chemical structure of formula I, wherein n is 0 or 1, X is N or C-R1, R1 is H or Cl, R2 and R3 are independently H, a halogen or an alkyl group, Ar is a substituted or unsubstituted phenylene or naphthylene group, with the substituted or unsubstituted phenylene group being A or B, and the naphthylene group being C, R4 is H, a halogen or an alkyl group, R5 is H, a halogen, an alkyl group, an alkoxyl group or a hydroxyl group, R6 is H or a hydroxyl group, and R7 is a substituted or unsubstituted aryl group. The compound has SHP-1 agonist activity, and can be used to treat cancer.
Antischistosomal activity of N,N′-arylurea analogs against Schistosoma japonicum
Yao, Houzong,Liu, Fengyou,Chen, Jinglei,Li, Yan,Cui, Jinhao,Qiao, Chunhua
supporting information, p. 1386 - 1390 (2016/02/19)
Although the antischistosomal activities of N,N′-arylurea analogs were reported, systematic structure-activity relationships have not been conducted. In this Letter, we reported the design, synthesis and evaluation of 45 N,N′-arylurea analogs. Among these prepared compounds, 13 compounds were urea linker modified and 32 were N,N′-arylurea derivatives. The activity evaluation revealed 12 analogs exhibited IC50 values lower than 22.6 μM, and 7 of them had IC50 less than 10 μM against the juvenile Schistosoma japonicum in vitro. Their worm killing potency was even higher against adult worm. Unfortunately, low to moderate worm burden reduction of 0-33.4% was recorded after administration of a single oral dose of 200 mg/kg or 400 mg/kg to mice harboring S. japonicum.
In vitro inhibition of translation initiation by N,N′-diarylureas - Potential anti-cancer agents
Denoyelle, Séverine,Chen, Ting,Chen, Limo,Wang, Yibo,Klosi, Edvin,Halperin, José A.,Aktas, Bertal H.,Chorev, Michael
supporting information; experimental part, p. 402 - 409 (2012/02/04)
Symmetrical N,N′-diarylureas: 1,3-bis(3,4-dichlorophenyl)-, 1,3-bis[4-chloro-3-(trifluoromethyl)phenyl]- and 1,3-bis[3,5- bis(trifluoromethyl)phenyl]urea, were identified as potent activators of the eIF2α kinase heme regulated inhibitor. They reduce the abundance of the eIF2·GTP·tRNAiMet ternary complex and inhibit cancer cell proliferation. An optimization process was undertaken to improve their solubility while preserving their biological activity. Non-symmetrical hybrid ureas were generated by combining one of the hydrophobic phenyl moieties present in the symmetrical ureas with the polar 3-hydroxy-tolyl moiety. O-alkylation of the later added potentially solubilizing charge bearing groups. The new non-symmetrical N,N′-diarylureas were characterized by ternary complex reporter gene and cell proliferation assays, demonstrating good bioactivities. A representative sample of these compounds potently induced phosphorylation of eIF2α and expression of CHOP at the protein and mRNA levels. These inhibitors of translation initiation may become leads for the development of potent, non-toxic, and target specific anti-cancer agents.
