137844-98-5Relevant articles and documents
Syntheses, crystal structures, thermal stabilities, CT-DNA, and BSA binding characteristics of a new acylhydrazone and its Co(II), Cu(II), and Zn(II) complexes
Liu, Jing-Jing,Liu, Xiang-Rong,Zhao, Shun-Sheng,Yang, Zai-Wen,Yang, Zheng
, p. 1159 - 1176 (2020)
A new acylhydrazone (C12H12N4OS, HL) and its three transition metal complexes [M(HL)2](NO3)2 (M = Co, I; Cu, II; Zn, III) have been synthesized. The structures of above four compounds were determined by single-crystal X-ray diffraction analyses. HL belonged to orthorhombic system and Pbca space group. I and II belonged to triclinic system and P-1 space group, whereas III belonged to monoclinic system and P21/C space group. The thermal stabilities of four compounds were investigated by thermogravimetric analyses, and their maximum thermal decomposition peak temperatures were all more than 240 °C, showing high thermal stabilities. The binding behaviors of four compounds with CT-DNA were determined by UV–vis absorption spectra, viscosity and microcalorimetric experiments, all presenting intercalative modes. The interactions of four compounds with BSA were determined by fluorescence spectra and microcalorimetric experiments, showing static quenching effects, and the binding constants KA are (8.32 ± 0.36) × 103 M?1, (1.44 ± 0.40) × 105 M?1, (7.59 ± 0.09) × 104 M?1, and (4.68 ± 0.45) × 105 M?1 for HL, I, II, and III, respectively. Microcalorimetric experiments explored that the interactions of four compounds with CT-DNA or BSA were exothermic processes and the interaction times were all less than 43 min.
Synthesis and structure-activity relationship studies of 2-(1,3,4-oxadiazole-2(3H)-thione)-3-amino-5-arylthieno[2,3-b]pyridines as inhibitors of DRAK2
Leonczak, Piotr,Gao, Ling-Jie,Ramadori, Anna Teresa,Lescrinier, Eveline,Rozenski, Jef,De Jonghe, Steven,Herdewijn, Piet
, p. 2587 - 2601 (2015/04/22)
In recent years, DAPK-related apoptosis-inducing protein kinase 2 (DRAK2) has emerged as a promising target for the treatment of a variety of autoimmune diseases and for the prevention of graft rejection after organ transplantation. However, medicinal chemistry optimization campaigns for the discovery of novel small-molecule inhibitors of DRAK2 have not yet been published. Screening of a proprietary compound library led to the discovery of a benzothiophene analogue that displays an affinity constant (Kd) value of 0.25 μM. Variation of the core scaffold and of the substitution pattern afforded a series of 5-arylthieno[2,3-b]pyridines with strong binding affinity (Kd=0.008 μM for the most potent representative). These compounds also show promising activity in a functional biochemical DRAK2 enzyme assay, with an IC50 value of 0.029 μM for the most potent congener. Selectivity profiling of the most potent compounds revealed that they lack selectivity within the DAPK family of kinases. However, one of the less potent analogues is a selective ligand for DRAK2 and can be used as starting point for the synthesis of selective and potent DRAK2 inhibitors.
3-Aminothiophene-2-acylhydrazones: Non-toxic, analgesic and anti-inflammatory lead-candidates
Da Silva, Yolanda Karla Cupertino,Reyes, Christian Tadeo Moreno,Rivera, Gildardo,Alves, Marina Amaral,Barreiro, Eliezer J.,Moreira, Magna Suzana Alexandre,Lima, Lidia Moreira
, p. 8456 - 8471 (2014/07/08)
Different chemotypes are described as anti-inflammatory. Among them the N-acylhydrazones (NAH) are highlighted by their privileged structure nature, being present in several anti-inflammatory drug-candidates. In this paper a series of functionalized 3-ami
