41927-17-7Relevant academic research and scientific papers
INHIBITORS OF ENL/AF9 YEATS
-
, (2021/06/26)
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
TREX1 INHIBITORS AND USES THEREOF
-
, (2022/01/04)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds for inhibiting three prime repair exonuclease 1 ("TREX1").
Syntheses and pharmacokinetic evaluations of four metabolites of 2-(4-(2-((1H-benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis-(methylthio)pyridin-3-yl)acetamide hydrochloride [K-604], an acyl-CoA:cholesterol O-acyltransferase-1 inhibi
Miura, Toru,Ohgiya, Tadaaki,Omichi, Kozo,Shibuya, Kimiyuki,Tsunenari, Yoshihiko
, (2020/04/27)
We synthesized and identified four metabolites of acyl-coenzyme A:cholesterol O-acyltransferase (ACAT)-1 inhibitor, K-604 (1). Two of the metabolites M1 and M2, were prepared from 1 using a combination reagent of hydrogen peroxide and sodium tungstate wit
DIHYDROBENZIMIDAZOLONES
-
, (2019/03/17)
The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.
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.
N-[2-AMINO-4-(PHENYLMETHOXY)PHENYL] AMIDES AND RELATED COMPOUNDS AS POTASSIUM CHANNEL MODULATORS
-
Page/Page column 17-18, (2008/12/07)
This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
2-ARYLCARBOXAMIDE-NITROGENEOUS HETEROCYCLE COMPOUND
-
Page/Page column 26, (2008/06/13)
A compound represented bv the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents -N-, -CH-, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.
Detecting Hg2+ ions with an ICT fluorescent sensor molecule: Remarkable emission spectra shift and unique selectivity
Wang, Jiaobing,Qian, Xuhong,Cui, Jingnan
, p. 4308 - 4311 (2007/10/03)
A fluorescent ratiometric Hg2+ ion sensor RMS, based on a coumarin platform coupled with a tetraamide receptor, is presented. This sensor, employing the ICT mechanism, could be used to specifically detect Hg 2+ ions in a neutral buff
METHOD FOR PRODUCING CYCLIC DIAMINE DERIVATIVE OR SALT THEREOF
-
Page/Page column 7, (2008/06/13)
The present invention is directed to a method for producing a cyclic diamine compound (3) or a salt thereof through the following scheme: (wherein Ar represents a phenyl group, a pyridyl group, or a pyrimidinyl group, any of which may have a substituent; X represents NH, S, or O; ring A represents a benzene ring or a pyridine ring, which may have a substituent; 1 represents an integer of 1 or 2; m represents an integer of 1 or 2; and n represents an integer of 1 to 6). The method enables synthesis of a cyclic diamine compound (3) or a salt thereof, which serves as an ACAT inhibitor, in an industrially useful manner.
Discovery and structure-activity relationship of the first non-pep tide competitive human glucagon receptor antagonists
Madsen, Peter,Knudsen, Lotte B.,Wiberg, Finn C.,Carr, Richard D.
, p. 5150 - 5157 (2007/10/03)
The first non-peptide competitive human glucagon receptor antagonist, 2-(benzimidazol-2ylthio)-l-(3,4-dihydroxyphenyl)-l-ethanone, NNC 92-1687 (2), is described. This antagonist has a binding affinity of 20 μM (ICso) and a functional Ki = 9.1 μM at the human glucagon receptor. A structure-activity relationship (SAR) was obtained on this compound, and the results show that only the benzimidazole part can be changed without complete loss of affinity. Analogues with tert-butyl or benzyloxy groups in the 5-position of the benzimidazole moiety were found to be equipotent or slightly more potent, all displaying binding affinities around 5-20 μM. Most of the changes to the catechol and the linker gave compounds without any affinity toward the human glucagon receptor. The 3-hydroxy group could, however, in the presence of a 4-hydroxy group be changed to a methoxy or a chloro group while retaining affinity.
