Are inhibitors of histone deacetylase 8 (HDAC8) effective in hematological cancers especially acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) …

SA Amin, S Khatun, S Gayen, S Das, T Jha - European Journal of Medicinal …, 2023 - Elsevier
Abstract Histone deacetylase 8 (HDAC8) aberrantly deacetylates histone and non-histone
proteins. These include structural maintenance of chromosome 3 (SMC3) cohesin protein …

2-Aminobenzothiazoles in anticancer drug design and discovery

G Huang, T Cierpicki, J Grembecka - Bioorganic chemistry, 2023 - Elsevier
Cancer is one of the major causes of mortality and morbidity worldwide. Substantial
research efforts have been made to develop new chemical entities with improved anticancer …

A therapeutic perspective of HDAC8 in different diseases: an overview of selective inhibitors

A Fontana, I Cursaro, G Carullo, S Gemma… - International Journal of …, 2022 - mdpi.com
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional
repression and chromatin condensation mechanisms by removing the acetyl moiety from …

Synthesis, antitumor, and apoptosis-inducing activities of novel 5-arylidenethiazolidine-2, 4-dione derivatives: histone deacetylases inhibitory activity and molecular …

A Hamdi, WM Elhusseiny, DIA Othman, A Haikal… - European Journal of …, 2022 - Elsevier
The antitumor activity of the newly synthesized 5-arylidenethiazolidine-2, 4-dione derivatives
18a–f and 19a–f was investigated, compared to doxorubicin (IC 50= 4.17–8.87 μM) and …

Integrated fragment-based drug design and virtual screening techniques for exploring the antidiabetic potential of thiazolidine-2, 4-diones: Design, synthesis and in …

S Gupta, GS Baweja, S Singh, M Irani, R Singh… - European Journal of …, 2023 - Elsevier
Diabetes mellitus is a metabolic disorder characterized by elevated blood sugar levels and
related complications. This study focuses on harnessing and integrating fragment-based …

Thiazolidin-2, 4-dione scaffold: an insight into recent advances as antimicrobial, antioxidant, and hypoglycemic agents

H Kumar, N Aggarwal, MG Marwaha, A Deep… - Molecules, 2022 - mdpi.com
Heterocyclic compounds containing nitrogen and sulfur, especially those in the thiazole
family, have generated special interest in terms of their synthetic chemistry, which is …

Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects

J Ru, Y Wang, Z Li, J Wang, C Ren, J Zhang - European Journal of …, 2023 - Elsevier
Histone deacetylases (HDACs) catalyze the hydrolysis of acetyl-l-lysine side chains in
histones and non-histones, which are key to epigenetic regulation in humans. Targeting …

Overview of class I HDAC modulators: Inhibitors and degraders

Z Huang, L Zeng, B Cheng, D Li - European Journal of Medicinal Chemistry, 2024 - Elsevier
Class I histone deacetylases (HDACs) are closely associated with the development of a
diverse array of diseases, including cancer, neurodegenerative disorders, HIV, and …

Contribution of Knoevenagel condensation products toward the development of anticancer agents: An updated review

R Tokala, D Bora, N Shankaraiah - ChemMedChem, 2022 - Wiley Online Library
Knoevenagel condensation is an entrenched, prevailing, prominent arsenal following
greener principles in the generation of α, β‐unsaturated ketones/carboxylic acids by …

Synthesis and in vitro antibacterial, antifungal, anti-proliferative activities of novel adamantane-containing thiazole compounds

ET Warda, MB El-Ashmawy, ESE Habib… - Scientific reports, 2022 - nature.com
Abstract A series of (Z)-N-(adamantan-1-yl)-3, 4-diarylthiazol-2 (3 H)-imines (5a-r) was
synthesized via condensation of 1-(adamantan-1-yl)-3-arylthioureas (3a-c) with various aryl …