Molecules, 2014 A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay.
Hong Chen +6 more
doaj +4 more sources
Synthesis and Antitumor Activity of Novel Arylpiperazine Derivatives Containing the Saccharin Moiety
Molecules, 2017 Prostate cancer is a major public health problem worldwide. For the development of potential anti-prostate cancer agents, a series of novel arylpiperazine derivatives containing the saccharin moiety based on previous studies was designed, synthesized ...
Hong Chen +5 more
doaj +4 more sources
Molecules, 2011 In this work, a series of arylpiperazine derivatives were synthesized and screened by in vivo pharmacological trials. Among the tested compounds, 2-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)-1-phenylethanone (18) and 2-(4-(2,3-dimethylphenyl)piperazin-
Guisen Zhang +5 more
doaj +4 more sources
Modeling key interactions between dopamine D2 receptor second extracellular loop and arylpiperazine ligands [PDF]
Journal of the Serbian Chemical Society, 2012 Second extracellular loop (ecl2) of dopamine (DA) D2 receptor is an essential part of dopaminergic ligands binding pocket. To form a part of the ligand binding surface it has to fold down into the transmembrane domain of the DA receptor.
Šukalović Vladimir +4 more
doaj +3 more sources
Synthesis of Some New Thiazole Derivatives and Their Biological Activity Evaluation
Journal of Chemistry, 2015 New 2-(4-arylpiperazine-1-yl)-N-[4-(2-(4-substituted phenyl)thiazol-4-yl)phenyl]acetamide derivatives were synthesized and evaluated for their antimicrobial and anticholinesterase activities.
Leyla Yurttaş +3 more
doaj +2 more sources
Synthesis, bioactivity, and molecular docking studies: novel arylpiperazine derivatives as potential new-resistant AR antagonists [PDF]
Frontiers in ChemistryThe majority of patients with androgen-dependent prostate cancer (PCa) develop resistance to hormone therapy after approximately 18–24 months of androgen deprivation therapy treatment.
Hua Jiang +4 more
doaj +2 more sources
Photocatalysis and Kinetic Resolution by Lithiation to Give Enantioenriched 2-Arylpiperazines. [PDF]
Org Lett, 2023 Piperazines are important heterocycles in drug compounds. We report the asymmetric synthesis of arylpiperazines by photocatalytic decarboxylative arylation (metallaphotoredox catalysis) then kinetic resolution using n-BuLi/(+)-sparteine. This gave a range of piperazines with very high enantioselectivities.
Das A, Choi A, Coldham I.
europepmc +4 more sources
Design and Synthesis of a Novel 4-aryl-N-(2-alkoxythieno [2,3-b]pyrazine-3-yl)-4-arylpiperazine-1-carboxamide DGG200064 Showed Therapeutic Effect on Colon Cancer through G2/M Arrest [PDF]
Pharmaceuticals, 2022 Cancer cells are characterized by an abnormal cell cycle. Therefore, the cell cycle has been a potential target for cancer therapeutic agents. We developed a new lead compound, DGG200064 (7c) with a 2-alkoxythieno [2,3-b]pyrazine-3-yl)-4-arylpiperazine-1-
Eun-Sil Lee +9 more
doaj +2 more sources
New N-Arylpiperazine-Based Compounds as Potential Inhibitors of Purinergic P2X7-Associated Signaling [PDF]
LifeThis research paper focused on the synthesis of 1-[2-hydroxy-3-(phenylcarbamoyloxy)propyl]-4-(R1, R2-substituted phenyl)piperazin-1-ium chlorides (I)–(III), containing R1, R2 = H, Cl and/or OCH3, and the evaluation of some of their physicochemical ...
Gabriela Greifová +8 more
doaj +2 more sources
Heat Shock Proteins HSPA1 and HSP90AA1 Are Upregulated in Colorectal Polyps and Can Be Targeted in Cancer Cells by Anti-Inflammatory Oxicams with Arylpiperazine Pharmacophore and Benzoyl Moiety Substitutions at Thiazine Ring [PDF]
Biomolecules, 2021 Heat shock proteins HSPA1/Hsp70α and HSP90AA1/Hsp90α are crucial for cancer growth but their expression pattern in colorectal polyps or whether they can be modulated by oxicams is unknown.
Izabela Szczuka +4 more
doaj +2 more sources