In vitro inhibition of translation initiation by N, N′-diarylureas—potential anti-cancer agents

S Denoyelle, T Chen, L Chen, Y Wang, E Klosi…

Index: Denoyelle, Severine; Chen, Ting; Chen, Limo; Wang, Yibo; Klosi, Edvin; Halperin, Jose A.; Aktas, Bertal H.; Chorev, Michael Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 402 - 409

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Citation Number: 20

Abstract

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 ...