5-Ene-4-thiazolidinones–An efficient tool in medicinal chemistry

D Kaminskyy, A Kryshchyshyn, R Lesyk - European journal of medicinal …, 2017 - Elsevier
The presented review is an attempt to summarize a huge volume of data on 5-ene-4-
thiazolidinones being a widely studied class of small molecules used in modern organic and …

Rhodanine as a privileged scaffold in drug discovery

T Tomasic, LP Masic - Current Medicinal Chemistry, 2009 - ingentaconnect.com
Rhodanines, thiazolidine-2, 4-diones and pseudothiohydantoins have become a very
interesting class of heterocyclic compounds since the introduction of various glitazones and …

Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor

EM Bowers, G Yan, C Mukherjee, A Orry, L Wang… - Chemistry & biology, 2010 - cell.com
The histone acetyltransferase (HAT) p300/CBP is a transcriptional coactivator implicated in
many gene regulatory pathways and protein acetylation events. Although p300 inhibitors …

Recent developments with rhodanine as a scaffold for drug discovery

D Kaminskyy, A Kryshchyshyn… - Expert Opinion on Drug …, 2017 - Taylor & Francis
Introduction: Rhodanines, as one of the 4-thiazolidinones subtypes, are recognized as
privileged heterocycles in medicinal chemistry. The main achievements include the …

Virtual screening: a fast tool for drug design

V Vyas, A Jain, A Jain, A Gupta - Scientia Pharmaceutica, 2008 - mdpi.com
Computational screening of databases has become increasingly popular in the
pharmaceutical research. Virtual screening uses computer based methods to discover new …

Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo [h] quinoline scaffolds as anticancer agents

V Ramesh, BA Rao, P Sharma, B Swarna… - European Journal of …, 2014 - Elsevier
Abstract Several rhodanine derivatives (9–39) were synthesized for evaluation of their
potential as anticancer agents. Villsmeier cyclization to synthesize aza-aromatic aldehydes …

Selective small molecule inhibition of poly (ADP-ribose) glycohydrolase (PARG)

KE Finch, CE Knezevic, AC Nottbohm… - ACS chemical …, 2012 - ACS Publications
The poly (ADP-ribose)(PAR) post-translational modification is essential for diverse cellular
functions, including regulation of transcription, response to DNA damage, and mitosis …

Flavonoids inhibit both rice and sheep serotonin N‐acetyltransferases and reduce melatonin levels in plants

K Lee, OJ Hwang, RJ Reiter… - Journal of pineal …, 2018 - Wiley Online Library
The plant melatonin biosynthetic pathway has been well characterized, but inhibitors of
melatonin synthesis have not been well studied. Here, we found that flavonoids potently …

Targeting lysine acetylation readers and writers

MM Zhou, PA Cole - Nature Reviews Drug Discovery, 2024 - nature.com
Lysine acetylation is a major post-translational modification in histones and other proteins
that is catalysed by the 'writer'lysine acetyltransferases (KATs) and mediates interactions …

Rhodanine carboxylic acids as novel inhibitors of histone acetyltransferases

SD Furdas, S Shekfeh, S Kannan, W Sippl, M Jung - MedChemComm, 2012 - pubs.rsc.org
Histone acetyltransferases (HATs) are promising epigenetic drug targets and are involved in
the pathogenesis of a wide range of diseases. We carried out a virtual screening based on …