758711-89-6Relevant academic research and scientific papers
N,N′-diarylurea compounds and N,N′-diarylthiourea compounds as inhibitors of translation initiation
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, (2016/09/26)
Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.
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
, 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.
Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
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, (2008/06/13)
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
