[PDF][PDF] Synthesis, reactions, and applications of hydantoin and 2-thiohydantoin derivatives

H Abd Elhady, S El Desoky… - Acta Poloniae …, 2019 - bibliotekanauki.pl
On account of the interesting pharmacological properties of hydantoin and 2-thiohydantoin
derivatives, and other purposes such as textile printing, catalysts for polymerizations, their …

Design and synthesis of indoline thiohydantoin derivatives based on enzalutamide as antiproliferative agents against prostate cancer

M Zuo, X Xu, Z Xie, R Ge, Z Zhang, Z Li… - European journal of …, 2017 - Elsevier
A novel scaffold of indoline thiohydantoin was discovered as potent androgen receptor (AR)
antagonist through rational drug designation. Several compounds showed good biological …

Length-Dependent Transition from Extended to Folded Shapes in Short Oligomers of an Azetidine-Based α-Amino Acid: The Critical Role of NH··· N H-Bonds

D Liu, JX Bardaud, Z Imani, S Robin, E Gloaguen… - Molecules, 2023 - mdpi.com
Hydrogen bonds (H-bonds) are ubiquitous in peptides and proteins and are central to the
stabilization of their structures. Inter-residue H-bonds between non-adjacent backbone …

Use of the hydantoin directing group in ruthenium (II)-catalyzed C–H functionalization

JA Leitch, HP Cook, Y Bhonoah… - The Journal of Organic …, 2016 - ACS Publications
Ruthenium (II)-catalyzed C–H functionalization of N-arylhydantoins is herein described. The
biologically relevant hydantoin (imidazolidinedione) heterocycle functions as a weakly …

The design, synthesis and anti-tumor mechanism study of new androgen receptor degrader

H Xie, JJ Liang, YL Wang, TX Hu, JY Wang… - European Journal of …, 2020 - Elsevier
Targeted protein degradation using small molecules is a novel strategy for drug
development. In order to solve the problem of drug resistance in the treatment of prostate …

Discovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants

J Yu, P Zhou, M Hu, L Yang, G Yan, R Xu… - European Journal of …, 2019 - Elsevier
Androgen receptor (AR) has been a target of prostate cancer (PC) for nearly six decades.
Recently, downregulating or degrading AR and the mutants especially the splice variant 7 …

Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents

X Xu, R Ge, L Li, J Wang, X Lu, S Xue, X Chen… - European Journal of …, 2018 - Elsevier
Prostate cancer (PC) is a major cause of cancer-related male death in worldwide and the
identification of new and improved potent anti-PC molecules is constantly required. A novel …

Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation

Q Tang, W Fu, M Zhang, E Wang, L Shan… - European Journal of …, 2020 - Elsevier
Androgen receptor (AR) plays important roles in the development of prostate cancer (PCa),
and therefore it has been regarded as the most important therapeutic target for both …

Discovery of Novel Anti‐Resistance AR Antagonists Guided by Funnel Metadynamics Simulation

H Chen, Y Zhou, X Wang, X Chai, Z Wang… - Advanced …, 2024 - Wiley Online Library
Androgen receptor (AR) antagonists are widely used for the treatment of prostate cancer
(PCa), but their therapeutic efficacy is usually compromised by the rapid emergence of drug …

Synthesis, crystal structure, DFT studies, acid dissociation constant, and antimicrobial activity of methyl 2-(4-chlorophenyl)-7a-((4-chlorophenyl) carbamothioyl)-1-oxo …

Y Nural, M Gemili, N Seferoglu, E Sahin, M Ulger… - Journal of Molecular …, 2018 - Elsevier
A novel bicyclic thiohydantoin fused to pyrrolidine compound, methyl 2-(4-chlorophenyl)-7a-
((4-chlorophenyl) carbamothioyl)-1-oxo-5, 5-diphenyl-3-thioxo-hexahydro-1H-pyrrolo [1, 2-e] …