Results 71 to 80 of about 957 (180)

The translational value of ligand‐receptor binding kinetics in drug discovery

British Journal of Pharmacology, Volume 181, Issue 21, Page 4117-4129, November 2024.
Abstract The translation of in vitro potency of a candidate drug, as determined by traditional pharmacology metrics (such as EC50/IC50 and KD/Ki values), to in vivo efficacy and safety is challenging. Residence time, which represents the duration of drug‐target interaction, can be part of a more comprehensive understanding of the dynamic nature of drug‐
Hongli Liu, Haoran Zhang, Adriaan P. IJzerman, Dong Guo   +3 more
wiley   +1 more source

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Molecules, 2011
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically ...
William L. Scott, Ziniu Zhou, Martin J. O’Donnell, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Gaël Nomezine, Maciej Pawłowski, Gilles Subra, Katarzyna Grychowska, Joanna Król, Paweł Zajdel   +11 more
doaj   +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

Mechanistic study of novel arylpiperazine derivative NAF19 in prostate cancer treatment based on network pharmacology approach

Romanian Journal of Laboratory Medicine
Our preliminary studies identified the arylpiperazine derivative NAF19 as a promising therapeutic agent against prostate cancer, though its precise mechanisms remained unclear.
Jiang Hua, Xu Mingzhen, Jiang Songsong, Huang Weiqiang, Chen Hong   +4 more
doaj   +1 more source

Data for: Synthesis and pharmacological evaluation of novel arylpiperazine oxicams derivatives as potent analgesics without ulcerogenicity

, 2019
Data for: Synthesis and pharmacological evaluation of novel arylpiperazine oxicams derivatives as potent analgesics without ulcerogenicityTHIS DATASET IS ARCHIVED AT DANS/EASY, BUT NOT ACCESSIBLE HERE. TO VIEW A LIST OF FILES AND ACCESS THE FILES IN THIS
Szczęśniak-Sięga, B (via Mendeley Data)
core   +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

In silico studies of piperazine derivatives as potent anti-proliferative agents against PC-3 prostate cancer cell lines

Heliyon, 2020
Quantitative Structure Activity Relationship studies were carried out on arylpiperazine derivatives to investigate their anti-proliferate activity against prostate PC-3 cancer cell lines.
Fabian A. Ikwu, Gideon A. Shallangwa, Paul A. Mamza, Adamu Uzairu   +3 more
doaj   +1 more source

Coumarin-piperazine derivatives as biologically active compounds

Saudi Pharmaceutical Journal, 2020
A number of psychiatric disorders, including anxiety, schizophrenia, Parkinson’s disease, depression and others CNS diseases are known to induce defects in the function of neural pathways sustained by the neurotransmitters, like dopamine and serotonin. N-
Kinga Ostrowska
doaj   +1 more source

Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands

Chemistry Central Journal, 2018
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated.
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J. Bojarski, Joachim Kusz, Paweł Zajdel   +8 more
doaj   +1 more source

Design and synthesis of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazole derivatives as colchicine binding site inhibitors

, 2017
A series of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazol derivatives were designed as potential microtubule targeting agents. The regioselective alkylation of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazole was predicted by ...
Kai Bao, Peng Yan, Weige Zhang, Daiying Zuo, Qi Guan, Yue Wu, Meiqi Gao, Zhiwei Wang, Jun Sun, Yingliang Wu, Dongjie Feng, Zhenzhen Gu   +11 more
core   +1 more source