16634-82-5Relevant articles and documents
An Expedient Process for the Synthesis of 2-(N -Arylamino)benzaldehydes from 2-Hydroxybenzaldehydes via Smiles Rearrangement
Saeidian, Hamid,Mirjafary, Zohreh,Abdolmaleki, Elinaz,Moradnia, Farzaneh
, p. 2127 - 2131 (2013)
This paper describes an efficient Smiles rearrangement process for the synthesis of 2-(N-arylamino)benzaldehyde derivatives with reasonable yields. A mechanism is proposed for the reaction course. Georg Thieme Verlag Stuttgart, New York.
Design, synthesis, docking study, α-glucosidase inhibition, and cytotoxic activities of acridine linked to thioacetamides as novel agents in treatment of type 2 diabetes
Mohammadi-Khanaposhtani, Maryam,Rezaei, Sepideh,Khalifeh, Reza,Imanparast, Somaye,Faramarzi, Mohammad Ali,Bahadorikhalili, Saeed,Safavi, Malihe,Bandarian, Fatemeh,Nasli Esfahani, Ensieh,Mahdavi, Mohammad,Larijani, Bagher
, p. 288 - 295 (2018)
A novel series of acridine linked to thioacetamides 9a–o were synthesized and evaluated for their α-glucosidase inhibitory and cytotoxic activities. All the synthesized compounds exhibited excellent α-glucosidase inhibitory activity in the range of IC50 = 80.0 ± 2.0–383.1 ± 2.0 μM against yeast α-glucosidase, when compared to the standard drug acarbose (IC50 = 750.0 ± 1.5 μM). Among the synthesized compounds, 2-((6-chloro-2-methoxyacridin-9-yl)thio)-N-(p-tolyl) acetamide 9b displayed the highest α-glucosidase inhibitory activity (IC50 = 80.0 ± 2.0 μM). The in vitro cytotoxic assay of compounds 9a–o against MCF-7 cell line revealed that only the compounds 9d, 9c, and 9n exhibited cytotoxic activity. Cytotoxic compounds 9d, 9c, and 9n did not show cytotoxic activity against the normal human cell lines HDF. Kinetic study revealed that the most potent compound 9b is a competitive inhibitor with a Ki of 85 μM. Furthermore, the interaction modes of the most potent compounds 9b and 9f with α-glucosidase were evaluated through the molecular docking studies.
Synthesis and luminescence properties of 1,3,4-oxadiazole acetamide derivatives and their rare earth complexes
Zhang, Wu,He, Wei,Guo, Xiaorui,Chen, Yanwen,Wu, Limin,Guo, Dongcai
, p. 383 - 389 (2015)
A series of 1,3,4-oxadiazole acetamide derivatives have been designed and synthesized, and their complexes with Eu(III) and Tb(III) were also prepared. The luminescence properties of the target complexes were investigated, and the results indicated that a
Optimization of pyrrolizine-based Schiff bases with 4-thiazolidinone motif: Design, synthesis and investigation of cytotoxicity and anti-inflammatory potency
Shawky, Ahmed M.,Abourehab, Mohammed A.S.,Abdalla, Ashraf N.,Gouda, Ahmed M.
, (2020)
Two new series of pyrrolizine-5-carboxamides were synthesized and evaluated for their anticancer and anti-inflammatory activities. The new compounds exhibited potent cytotoxicity (IC50 = 0.10–22.96 μM) against three cancer (MCF-7, A2780 and HT2
Synthesis, characterization and properties of salicylhydrazide-salicylacylhydrazone derivatives and their terbium complexes
Meng, Defen,Liu, Fen,Li, Yingying,Yang, Zehui,Li, Guizhi,Guo, Dongcai
, p. 507 - 514 (2016)
A series of terbium complexes with salicylhydrazide-salicylacylhydrazone derivatives were synthesized and characterized by elemental analysis, IR spectra, UV/vis spectra and thermal analysis. The luminescence and electrochemical properties of the terbium complexes were investigated. The results show that all the target complexes exhibited characteristic emissions of terbium ions and the complex substituted by the chlorine has the strongest luminescence intensity with the highest quantum yield at 0.609. The introduction of donating electron groups could increase the oxidation potential and the highest occupied molecular orbital energy level of the terbium complex; however, the introduction of accepting electron groups gave the opposite result.
Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents
Shawky, Ahmed M.,Ibrahim, Nashwa A.,Abdalla, Ashraf N.,Abourehab, Mohammed A. S.,Gouda, Ahmed M.
, p. 1313 - 1333 (2021)
In the present study, two new series of pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety were designed, synthesised, and evaluated for their cytotoxic activity. The benzamide derivatives 16a–e showed higher cytotoxicity than their corresponding Schiff b
Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein
Chen, Kaixian,Chen, Zhifeng,Dang, Yongjun,Ding, Hong,Fan, Shijie,Hu, Junchi,Jiang, Hualiang,Li, Lianchun,Li, Quanfu,Lin, Tingting,Lu, Junyan,Luo, Cheng,Otomo, Chinatsu,Otomo, Takanori,Tan, Minjia,Tao, Hongru,Wan, Wei,Wen, Yi,Xie, Yuli,Xu, Pan,Yao, Zhiyi,Yue, Liyan,Zhang, Bidong,Zhang, Naixia,Zhang, Yuanyuan,Zhou, Bing,Zhu, Mingrui
supporting information, p. 26105 - 26114 (2021/11/09)
The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins, including autophagy receptors, which stands out as a promising protein–protein interaction (PPI) target for the intervention of autophagy. Post-translational modifications like acetylation of Lys49 on the LIR-interacting surface could disrupt the interaction, offering an opportunity to design covalent small molecules interfering with the interface. Through screening covalent compounds, we discovered a small molecule modulator of LC3A/B that covalently modifies LC3A/B protein at Lys49. Activity-based protein profiling (ABPP) based evaluations reveal that a derivative molecule DC-LC3in-D5 exhibits a potent covalent reactivity and selectivity to LC3A/B in HeLa cells. DC-LC3in-D5 compromises LC3B lipidation in vitro and in HeLa cells, leading to deficiency in the formation of autophagic structures and autophagic substrate degradation. DC-LC3in-D5 could serve as a powerful tool for autophagy research as well as for therapeutic interventions.
Antidiabetic compounds
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Page/Page column 13-14, (2020/06/16)
Compounds for the treatment of hyperglycemia and/or diabetes are provided. The compounds, which inhibit the enzyme dipeptidyl peptidase (DPP-4), are based on the structure where X may be present or absent an may be OH, Ar is an aryl group; and n ranges from 0 to 5.