Results 41 to 50 of about 1,055 (154)

Synthesis of I-arylpiperazine-4-thiocarboxamides

, 1969
The reaction of 1-arylpiperazine salts with hot aqueous ammonium thiocyanate for a short time affords only the thiocyanate salts. l-Arylpiperazine-4-thiocarboxamides have been obtained by prolonged heating of the aqueous solutions of the thiocyanate ...
Ghate, S. P., Arya, V. P., Venkateswarlu, A., Nagarajan, K.   +3 more
core   +1 more source

TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer

Molecular Oncology, Volume 18, Issue 8, Page 1980-2000, August 2024.
The androgen receptor (AR) antagonist TAS3681 is effective against AR mutations, which leads to agonistic activity of AR signal inhibitors, and had an antitumor effect in an AR‐splice variant 7 (AR‐V7)‐positive enzalutamide‐resistant xenograft model. TAS3681 suppresses aberrant AR activation, including AR overexpression and expression of constitutively
Shohei Yoshida, Daisuke Kajiwara, Masanao Seki, Manabu Tayama, Yuki Tanaka, Hiroya Mizutani, Ryoto Fujita, Keisuke Yamamura, Shigeo Okajima, Masanori Asai, Kazuhisa Minamiguchi   +10 more
wiley   +1 more source

Molecular Modeling of 5HT(2A) Receptor - Arylpiperazine Ligands Interactions

, 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 ...
Kostić Rajačić, Slađana, Šukalović, Vladimir, Shakib, Kaveh, Senćanski, Milan, Došen-Mićović, Ljiljana, Šoškić, Vukić   +5 more
core   +1 more source

Poster Sessions

HemaSphere, Volume 10, Issue S1, June 2026.
wiley   +1 more source

Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands

, 2010
An easy and convenient microwave-assisted synthesis of a small library of indolic arylpiperazine derivatives is described. Parallel and mixed pool combinatorial methods are reported and compared.
FIORINO F., MAGLI E., ESPOSITO A., FRECENTESE F., SEVERINO B., PERISSUTTI E., SANTAGADA V., CALIENDO G., MASSARELLI P., DE ANGELIS F., NENCINI C., VITI B.   +11 more
core   +2 more sources

Exploration of N-arylpiperazine Binding Sites of D2 Dopaminergic Receptor

, 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   +1 more source

Synthesis of Arylpiperazine Derivatives as Protease Activated Receptor 1 Antagonists and Their Evaluation as Antiproliferative Agents

, 2017
Background: Protease activated receptor-1 (PAR1) is a G-coupled receptor activated by α-thrombin and other proteases. Several reports have demonstrated the PAR1 involvement in tumorigenesis and tumor progression.
CORVINO, ANGELA, Zotti, Andrea Ilaria, CALIENDO, GIUSEPPE, PERISSUTTI, ELISA, CIRINO, GIUSEPPE, MAGLI, ELISA, FRECENTESE, FRANCESCO, Terranova Barberio, Manuela, Di Gennaro, Elena, SEVERINO, BEATRICE, Iannelli, Federica, SANTAGADA, VINCENZO, FIORINO, FERDINANDO, ROVIEZZO, FIORENTINA, BUDILLON, Alfredo   +14 more
core   +1 more source

4-Azatricyclo[5.2.2.02,6]undecane-3,5,8-triones as Potential Pharmacological Agents

, 2008
A series of twenty six arylpiperazine and aminoalkanol derivatives of 4-azatricyclo[ 5.2.2.02,6]undecane-3,5,8-trione have been prepared.
Izabela Dybała, Marta Struga, Jerzy Kossakowski, Anna E. Kozioł, Izabela Dybała, Barbara Mirosław, Barbara Mirosław, Anna E. Kozioł, Anna Bielenica   +8 more
core   +1 more source

Imidazoles as Serotonin Receptor Modulators for Treatment of Depression: Structural Insights and Structure-Activity Relationship Studies. [PDF]

Pharmaceutics, 2023
Goel KK, Thapliyal S, Kharb R, Joshi G, Negi A, Kumar B.   +5 more
europepmc   +1 more source

Molecular modeling study of 4-phenylpiperazine and 4-phenyl-1,2,3,6-tetrahydropyridine derivatives: A new step towards the design of high-affinity 5-HT1A ligands

, 2010
peer reviewedThe main feature of many drugs having a 5-HT1A affinity is the presence of an arylpiperazine moiety. Indeed, the protonated nitrogen and the aromatic ring of the arylpiperazine compounds are considered crucial for the interaction with the ...
Graulich, Amaury, Liégeois, Jean-François, Dilly, Sébastien, Amaury Graulich, Jean-François Liégeois, Sébastien Dilly   +5 more
core   +1 more source