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 …

Hydrazides as Inhibitors of Histone Deacetylases

MC Carreiras, J Marco-Contelles - Journal of Medicinal Chemistry, 2024 - ACS Publications
In this Perspective, we have brought together available biological evidence on hydrazides
as histone deacetylase inhibitors (HDACis) and as a distinct type of Zn-binding group (ZBG) …

Selective HDAC3 inhibitors with potent in vivo Antitumor Efficacy against Triple-negative breast Cancer

S Pulya, A Himaja, M Paul, N Adhikari… - Journal of Medicinal …, 2023 - ACS Publications
HDAC3 modulation shows promise for breast cancer, including triple-negative cases. Novel
pyrazino-hydrazide-based HDAC3 inhibitors were designed and synthesized. Lead …

Concurrent delivery of Paclitaxel and Chlorin e6 to tumors using Albumin/PLGA nanoparticles for NIR Light-Triggered Chemo/Photodynamic therapy

M Paul, H Bhatt, S Kumbham, B Ghosh… - ACS Applied Nano …, 2023 - ACS Publications
In an attempt to develop a nanomedicine with the ability to produce combination chemo-and
photodynamic therapeutic effects in cancer, herein, we fabricated poly (d, l-lactic-co-glycolic …

Design, synthesis, and biological evaluation of tetrahydroisoquinoline based hydroxamate derivatives as HDAC 6 inhibitors for cancer therapy

YM Khetmalis, B Shree, BVS Kumar… - Journal of Molecular …, 2023 - Elsevier
A series of novel tetrahydroisoquinoline (THIQ) compounds were synthesized and evaluated
as histone deacetylase 6 (HDAC 6) inhibitors. The compounds are designed based on …

Fragment-based structural exploration and chemico-biological interaction study of HDAC3 inhibitors through non-linear pattern recognition, chemical space, and …

S Banerjee, S Dumawat, T Jha, G Lanka… - Journal of …, 2024 - Taylor & Francis
HDAC3 is an emerging target for the identification and discovery of novel drug candidates
against several disease conditions including cancer. Here, a fragment-based non-linear …

Human Serum Albumin-Oxaliplatin (Pt (IV)) prodrug nanoparticles with dual reduction sensitivity as effective nanomedicine for triple-negative breast cancer

M Paul, B Ghosh, S Biswas - International Journal of Biological …, 2024 - Elsevier
Nanomedicines have emerged as a potential strategy to reduce the toxic effect of drugs
administered via conventional approaches. Nanomedicines undergo passive and active …

Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects

Z Sun, C Xu, J Cheng, Z Yang, T Liu… - Journal of Medicinal …, 2024 - ACS Publications
Targeting the programmed cell death-1/ligand 1 (PD-1/PD-L1) pathway is one of the most
promising cancer treatment strategies. Studies have shown that HDAC inhibitors can …

Synthesis and antiproliferative potency of 1, 3, 4-thiadiazole and 1, 3-thiazolidine-4-one based new binary heterocyclic molecules: in vitro cell-based anticancer …

A Maji, A Himaja, S Nikhitha, S Rana, A Paul… - RSC Medicinal …, 2024 - pubs.rsc.org
Herein, we report the synthesis and anticancer properties of 21 new 1, 3, 4-thiadiazole-2-yl-
imino-thiazolidine-4-one containing binary heterocyclic molecules. Cytotoxicity of the …

HDAC3 inhibitors: a patent review of their broad-spectrum applications as therapeutic agents

TB Makgoba, E Kapp, S Egieyeh… - Expert Opinion on …, 2024 - Taylor & Francis
ABSTRACT Introduction Histone deacetylases (HDACs) are a class of zinc-dependent
enzymes. They maintain acetylation homeostasis, with numerous biological functions and …