An overview on applications of SwissADME web tool in the design and development of anticancer, antitubercular and antimicrobial agents: a medicinal chemist's …

B Bakchi, AD Krishna, E Sreecharan… - Journal of Molecular …, 2022 - Elsevier
Recently, in silico techniques have gained tremendous popularity in the field of small
molecule drug discovery. The computational jobs include not only hit generation, lead …

[HTML][HTML] Pathological role of HDAC8: cancer and beyond

JY Kim, H Cho, J Yoo, GW Kim, YH Jeon, SW Lee… - Cells, 2022 - mdpi.com
Histone deacetylase 8 (HDAC8) is a class I HDAC that catalyzes the deacetylation of histone
and non-histone proteins. As one of the best-characterized isoforms, numerous studies have …

[HTML][HTML] 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 …

[HTML][HTML] Significance of five-membered heterocycles in human histone deacetylase inhibitors

A Frühauf, M Behringer, FJ Meyer-Almes - Molecules, 2023 - mdpi.com
Five-membered heteroaromatic rings, in particular, have gained prominence in medicinal
chemistry as they offer enhanced metabolic stability, solubility and bioavailability, crucial …

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, 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 …

[HTML][HTML] Non-hydroxamate zinc-binding groups as warheads for histone deacetylases

A Frühauf, FJ Meyer-Almes - Molecules, 2021 - mdpi.com
Histone deacetylases (HDACs) remove acetyl groups from acetylated lysine residues and
have a large variety of substrates and interaction partners. Therefore, it is not surprising that …

Structure-based inhibitor discovery of class I histone deacetylases (HDACs)

Y Luo, H Li - International journal of molecular sciences, 2020 - mdpi.com
Class I histone deacetylases (HDACs) are promising targets for epigenetic therapies for a
range of diseases such as cancers, inflammations, infections and neurological diseases …

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation

N Upadhyay, K Tilekar, N Jänsch, M Schweipert… - Bioorganic …, 2020 - Elsevier
Epigenetics plays a fundamental role in cancer progression, and develo** agents that
regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs …

Synthesis, molecular modelling and pharmacological evaluation of novel indole-thiazolidinedione based hybrid analogues as potential pancreatic lipase inhibitors

G George, PS Auti, P Sengupta, N Yadav… - Journal of Biomolecular …, 2025 - Taylor & Francis
A series of novel indole-thiazolidinedione hybrid analogues (7a to 7 u) were synthesised,
characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst …