23249-97-0Relevant articles and documents
A unique 2D framework containing linear trimeric cobalt(ii) of mixed T d-Oh-Td geometries linked by two different single-carboxylate-aromatic amine ligands: Structure and magnetic properties
Yao, Min-Xia,Zeng, Ming-Hua,Zou, Hua-Hong,Zhou, Yan-Ling,Liang, Hong
, p. 2428 - 2432 (2008)
A new 2D coordination polymer Co3(OH)2(pa) 2(ina)2 (1, pa = 3-(1H-benzimidazol-2-yl) propanoic carboxylate, ina = isonicotinate) contained uncommon, linear Co(ii) trimers of mixed Td-Oh-Td geometries, exhibits spin canting below 20 K. Such magnetic behavior mainly arises from the Dzyaloshinski-Moriya interaction from the anisotropic, mixed geometries trimeric Co(ii) ions to the crimpled 2D network based on the nature of the binding modes of Co(ii)-carboxylate trimer and the effect of the intertrimers arrangement of 1. The mixed single-carboxylate-aromatic amine ligands bridged metal systems display a new structurally authenticated example of a thick 2D layer, and also indicate homometallic Co(ii) clusters with Td-Oh-T d mixed-geometries can result in relatively obvious noncompensation moments, according to different efficient spins of Co(ii) at very low temperature, in spite of antiferromagnetic intracluster interactions. The Royal Society of Chemistry.
An efficient synthesis of novel di-heterocyclic benzazole derivatives and evaluation of their antiproliferative activities
Algul, Oztekin,Ersan, Ronak Haj,Alagoz, Mehmet Abdullah,Duran, Nizami,Burmaoglu, Serdar
, p. 6926 - 6938 (2020/08/13)
A series of unsymmetrical nine di-heterocyclic compounds of benzazole derivatives were synthesized at one step via cyclization reaction. The compounds evaluated for in?vitro cytotoxic activity against A549, A498, HeLa, and HepG2 cancer cell lines. The biological evaluation results show that 23, 26 and 29 exhibit better activity against HepG2 and HeLa cancer cell lines. Compound 23 also showed good activity against A549, and A498 cancer cell lines. The analogs were further performed molecular docking studies against human cytochrome P450 2C8 monooxygenase enzyme, calculated some theoretical quantum parameters, ADMET descriptor and molecular electrostatic potential analysis. The strategy applied in this research work may act as a perspective for the rational design of potential anticancer drugs. Communicated by Ramaswamy H. Sarma.
Hit-to-Lead Optimization and Discovery of 5-((5-([1,1′-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase
Lan, Ping,Romero, F. Anthony,Wodka, Dariusz,Kassick, Andrew J.,Dang, Qun,Gibson, Tony,Cashion, Daniel,Zhou, Gaochao,Chen, Yuli,Zhang, Xiaoping,Zhang, Aihua,Li, Ying,Trujillo, Maria E.,Shao, Qing,Wu, Margaret,Xu, Shiyao,He, Huaibing,Mackenna, Deidre,Staunton, Jocelyn,Chapman, Kevin T.,Weber, Ann,Sebhat, Iyassu K.,Makara, Gergely M.
, p. 9040 - 9052 (2017/11/14)
AMP-activated protein kinase (AMPK) plays an essential role as a cellular energy sensor and master regulator of metabolism in eukaryotes. Dysregulated lipid and carbohydrate metabolism resulting from insulin resistance leads to hyperglycemia, the hallmark of type 2 diabetes mellitus (T2DM). While pharmacological activation of AMPK is anticipated to improve these parameters, the discovery of selective, direct activators has proven challenging. We now describe a hit-to-lead effort resulting in the discovery of a potent and selective class of benzimidazole-based direct AMPK activators, exemplified by 5-((5-([1,1′-biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic acid, 42 (MK-3903). Compound 42 exhibited robust target engagement in mouse liver following oral dosing, leading to improved lipid metabolism and insulin sensitization in mice.
