Designing multi-targeted agents: An emerging anticancer drug discovery paradigm

R Fu, Y Sun, W Sheng, D Liao - European journal of medicinal chemistry, 2017 - Elsevier
The dominant paradigm in drug discovery is to design ligands with maximum selectivity to
act on individual drug targets. With the target-based approach, many new chemical entities …

Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment

X Peng, Z Sun, P Kuang, J Chen - European Journal of Medicinal Chemistry, 2020 - Elsevier
Histone deacetylases (HDACs) are a class of enzymes that remove acetyl from the ε-N-
acetyl lysine of histones, allowing histones to wrap DNA more tightly. HDACs play an …

A review of progress in o-aminobenzamide-based HDAC inhibitors with dual targeting capabilities for cancer therapy

WX Zhang, J Huang, XY Tian, YH Liu, MQ Jia… - European journal of …, 2023 - Elsevier
Histone deacetylases, as a new class of anticancer targets, could maintain homeostasis by
catalyzing histone deacetylation and play important roles in regulating the expression of …

Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer

HM Hesham, DS Lasheen… - Medicinal Research …, 2018 - Wiley Online Library
Recently, molecular hybridization paradigm became an interesting and smart way to defeat
the multifaceted cancer disease by a single molecular entity that acts via several …

[HTML][HTML] Apigeninidin-rich Sorghum bicolor (L. Moench) extracts suppress A549 cells proliferation and ameliorate toxicity of aflatoxin B1-mediated liver and kidney …

SE Owumi, AI Kazeem, B Wu, LO Ishokare… - Scientific reports, 2022 - nature.com
Sorghum bicolor plant has a high abundance of 3-deoxyanthocyanins, flavonoids and other
polyphenol compounds that have been shown to offer numerous health benefits …

Distal Amidoketone Synthesis Enabled by Dimethyl Benziodoxoles via Dual Copper/Photoredox Catalysis

Y Ge, Y Shao, S Wu, P Liu, J Li, H Qin, Y Zhang… - ACS …, 2023 - ACS Publications
Herein, we report distal amidoketone and nitrogen-functionalized ketone syntheses from
alcohols and N–H nucleophiles enabled by hypervalent iodine dimethyl benziodoxoles …

Paradigm shift of “classical” HDAC inhibitors to “hybrid” HDAC inhibitors in therapeutic interventions

GN Vaidya, P Rana, A Venkatesh… - European journal of …, 2021 - Elsevier
Abstract 'Epigenetic'regulation of genes via post-translational modulation of proteins is the
current mainstay approach for the disease therapies, particularly explored in the Histone …

[HTML][HTML] HDAC3 Activity is Essential for Human Leukemic Cell Growth and the Expression of β-catenin, MYC, and WT1

M Beyer, A Romanski, AHM Mustafa, M Pons, I Büchler… - Cancers, 2019 - mdpi.com
Therapy of acute myeloid leukemia (AML) is unsatisfactory. Histone deacetylase inhibitors
(HDACi) are active against leukemic cells in vitro and in vivo. Clinical data suggest further …

Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors

J Chen, D Li, W Li, J Yin, Y Zhang, Z Yuan… - Bioorganic & medicinal …, 2018 - Elsevier
Multitarget inhibitors design has generated great interest in cancer treatment. Based on the
synergistic effects of topoisomerase and histone deacetylase inhibitors, we designed and …

A detail survey and analysis of selectivity criteria for indole-based histone deacetylase 8 (HDAC8) inhibitors

M Moinul, SA Amin, S Khatun, S Das, T Jha… - Journal of Molecular …, 2023 - Elsevier
Histone deacetylases (HDACs) are attractive therapeutic targets due to their involvement in
a variety of human diseases including cancer. All FDA-approved HDAC-targeting drugs are …