13940-96-0Relevant articles and documents
PqsR INVERSE AGONISTS
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Page/Page column 81-83, (2020/01/31)
The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
5 - [...] -2 alkyl substituted [...] and imidazole compound and use thereof
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Paragraph 0076-0078, (2018/05/07)
The present invention discloses a 5-aryl phenol-2 alkyl substituted urea benzimidazole compound and applications thereof, wherein the compound has a structure represented by a formula (I). According to the present invention, the 5-aryl phenol-2 alkyl subs
New benzimidazole-2-urea derivates as tubulin inhibitors
Wang, Wenna,Kong, Dexin,Cheng, Huimin,Tan, Li,Zhang, Zhang,Zhuang, Xiaoxi,Long, Huoyou,Zhou, Yang,Xu, Yong,Yang, Xiaohong,Ding, Ke
, p. 4250 - 4253 (2014/09/29)
Emerging drug resistance and other drawbacks limit tubulin inhibitors' therapeutic applications and developing novel tubulin inhibitors still attracts intensive efforts. We describe the discovery and structure-activity relationship study of a series of benzimidazole-2-urea derivatives as novel β tubulin inhibitors. The representative compound 6o potently suppressed the proliferation of a panel of human cancer cells (NCI-H460, Colo205, K562, A431, HepG2, Hela, MDA-MB-435S) with IC50 values of 0.040, 0.050, 0.006, 0.026, 1.774, 0.452 and 0.052 μM, respectively. Compound 6o obviously inhibited NCI-H460 spindles formation and induced cell cycle arrest at G2/M phase at 0.10 μM. Computational study suggested that 6o interacts with β tubulin in a novel binding mode. Our results suggested that benzimidazole-2-urea derivatives might be promising tubulin inhibitors with novel binding mode for further development.