Results 21 to 30 of about 957 (180)

Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
A series of 1-aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as microtubule destabilizers were designed, synthesised and evaluated for anticancer activity.
Chao Wang, Yuelin Li, Zi Liu, Zeyu Wang, Zihan Liu, Shuai Man, Yujing Zhang, Kai Bao, Yingliang Wu, Qi Guan, Daiying Zuo, Weige Zhang   +11 more
doaj   +2 more sources

Mechanism Exploration of Arylpiperazine Derivatives Targeting the 5-HT2A Receptor by In Silico Methods

Molecules, 2017
As a G-protein coupled receptor, the 5-hydroxytryptamine 2A (5-HT2A) receptor is known for its critical role in the cognitive, behavioural and physiological functions, and thus is a primary molecular target to treat psychiatric diseases, including ...
Feng Lin, Feng Li, Chao Wang, Jinghui Wang, Yinfeng Yang, Ling Yang, Yan Li   +6 more
doaj   +2 more sources

Interaction of arylpiperazine ligands with the hydrophobic part of the 5-HT1A receptor binding site

Bioorganic and Medicinal Chemistry, 2006
A flexible docking of a series of arylpiperazine derivatives with structurally different aryl part to the binding site of a model of human 5-HT1A receptor was exercised.
Mario Zlatovic, Vladimir Sukalovic, Göran Roglić   +2 more
exaly   +2 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, Nayeon Kim, Joon Hee Kang, Aizhan Abdildinova, Seon-Hyeong Lee, Myung Hwi Lee, Nam Sook Kang, Tae-Sung Koo, Soo-Youl Kim, Young-Dae Gong   +9 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, Jarosław Wierzbicki, Paweł Serek, Berenika M. Szczęśniak-Sięga, Małgorzata Krzystek-Korpacka   +4 more
doaj   +2 more sources

Synthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Despite the substantial clinical success of aspirin and clopidogrel in secondary prevention of ischemic stroke, up to 40% of patients remain resistant to the available antiplatelet treatment.
Monika Marcinkowska, Magdalena Kotańska, Agnieszka Zagórska, Joanna Śniecikowska, Monika Kubacka, Agata Siwek, Adam Bucki, Maciej Pawłowski, Marek Bednarski, Jacek Sapa, Małgorzata Starek, Monika Dąbrowska, Marcin Kołaczkowski   +12 more
doaj   +2 more sources

Exploration of N-arylpiperazine Binding Sites of D2 Dopaminergic Receptor

Mini-Reviews in Medicinal Chemistry, 2015
The crystal structures of the D3 dopamine receptor and several other G-protein coupled receptors (GPCRs) were published in recent times. Those 3D structures are used by us and other scientists as a template for the homology modeling and ligand docking ...
Kostić Rajačić, Slađana, Šukalović, Vladimir, Šoškić, Vukić   +2 more
core   +4 more sources

Arylpiperazine derivatives as serotoninergic ligands

, 2009
Serotonin is a neuromediator well known for its implication in mood regulation, anxiety, depression,insomnia as well as in normal human function such as sleep, sexual activity and appetite and recently it was demonstrated its involvement in the ...
SEVERINO B, MASSARELLI, PAOLA, SANTAGADA V, FIORINO F, FRECENTESE F, RENNER C, CALIENDO G., DE ANGELIS F, ESPOSITO A, PERISSUTTI E   +9 more
core   +2 more sources

Molecular Modeling of 5HT2AReceptor – Arylpiperazine Ligands Interactions

Chemical Biology and Drug Design, 2014
In this paper, we report the molecular modeling of the 5HT(2A) receptor and the molecular docking of arylpiperazine-like ligands. The focus of the research was on explaining the effects the ligand structure has on the binding properties of the 5HT(2A ...
Milan Senćanski, Vladimir Sukalovic, Kaveh Shakib   +2 more
exaly   +2 more sources

A novel arylpiperazine derivative (LQFM181) protects against neurotoxicity induced by 3- nitropropionic acid in in vitro and in vivo models [PDF]

Chemico-Biological Interactions
In the pursuit of novel antioxidant therapies for the prevention and treatment of neurodegenerative diseases, three new arylpiperazine derivatives (LQFM181, LQFM276, and LQFM277) were synthesized through a molecular hybridization approach involving ...
Hericles Mesquita Campos, Robbert Mota Pereira, Nkaa Uchenna   +2 more
exaly   +2 more sources