40516-96-9Relevant academic research and scientific papers
Synthesis, Chemical Characterization, and μ-Opioid Receptor Activity Assessment of the Emerging Group of "nitazene" 2-Benzylbenzimidazole Synthetic Opioids
Vandeputte, Marthe M.,Van Uytfanghe, Katleen,Layle, Nathan K.,St. Germaine, Danielle M.,Iula, Donna M.,Stove, Christophe P.
, p. 1241 - 1251 (2021/05/07)
Several 2-benzylbenzimidazole opioids (also referred to as "nitazenes") recently emerged on the illicit market. The most frequently encountered member, isotonitazene, has been identified in multiple fatalities since its appearance in 2019. Although recent
Design, synthesis and biological evaluation of novel 7-alkylamino substituted benzo[ a[phenazin derivatives as dual topoisomerase I/II inhibitors
Yao, Bing-Lei,Mai, Yan-Wen,Chen, Shuo-Bin,Xie, Hua-Ting,Yao, Pei-Fen,Ou, Tian-Miao,Tan, Jia-Heng,Wang, Hong-Gen,Li, Ding,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Zhi-Shu
, p. 540 - 553 (2015/01/30)
A novel series of benzo[a]phenazin derivatives bearing alkylamino side chains were designed, synthesized and evaluated for their topoisomerases inhibitory activity as well as cytotoxicity against four human cancer cell lines (HL-60, K-562, HeLa, and A549)
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity
Bressi, Jerome C.,Jong, Ron de,Wu, Yiqin,Jennings, Andy J.,Brown, Jason W.,O'Connell, Shawn,Tari, Leslie W.,Skene, Robert J.,Vu, Phong,Navre, Marc,Cao, Xiaodong,Gangloff, Anthony R.
scheme or table, p. 3138 - 3141 (2010/09/03)
A series of N-hydroxy-3-[3-(1-substituted-1H-benzoimidazol-2-yl)-phenyl]-acrylamides (5a-5ab) and N-hydroxy-3-[3-(1,4,5-trisubstituted-1H-imidazol-2-yl)-phenyl]-acrylamides (12a-s) were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases. Multiple compounds bearing an N1-piperidine demonstrate EC50s of 20-100 nM in human A549, HL60, and PC3 cells, in vitro and in vivo hyperacetylation of histones H3 and H4, and induction of p21waf. Compound 5x displays efficacy in human tumor xenograft models.
Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening
Holloway, Georgina A.,Baell, Jonathan B.,Fairlamb, Alan H.,Novello, Patrizia M.,Parisot, John P.,Richardson, John,Watson, Keith G.,Street, Ian P.
, p. 1422 - 1427 (2007/10/03)
A high-throughput screening campaign of a library of 100,000 lead-like compounds identified 2-iminobenzimidazoles as a novel class of trypanothione reductase inhibitors. These 2-iminobenzimidazoles display potent trypanocidal activity against Trypanosoma
