5625-68-3Relevant academic research and scientific papers
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)
BICYCLIC HETEROCYCLES CAPABLE OF MODULATING T-CELL RESPONSES, AND METHODS OF USING SAME
-
, (2014/01/07)
The present disclosure is directed in part to bicyclic heterocycles, such as a compound represented by formula (I) or (II) as disclosed herein, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulc
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
Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors
Dudash Jr., Joseph,Zhang, Yongzheng,Moore, John B.,Look, Richard,Liang, Yin,Beavers, Mary Pat,Conway, Bruce R.,Rybczynski, Philip J.,Demarest, Keith T.
, p. 4790 - 4793 (2007/10/03)
A series of 3-anilino-quinoxalinones has been identified as a new class of glycogen phosphorylase inhibitors. The lead compound 1 was identified through high throughput screening as well as through pharmacophore-based electronic screening. Modifications were made to the scaffold of 1 to produce novel analogues, some of which are 25 times more potent than the lead compound.
ARYL SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS SODIUM CHANNEL BLOCKERS
-
Page 25, (2008/06/13)
This invention relates aryl substituted benzimidazoles of Formula (I), or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also di
