Roles of histone deacetylases and inhibitors in anticancer therapy
Histones are the main structural proteins of eukaryotic chromatin. Histone acetylation/
deacetylation are the epigenetic mechanisms of the regulation of gene expression and are …
deacetylation are the epigenetic mechanisms of the regulation of gene expression and are …
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors
AKA Bass, MS El-Zoghbi, ESM Nageeb… - European journal of …, 2021 - Elsevier
Despite the encouraging clinical progress of chemotherapeutic agents in cancer treatment,
innovation and development of new effective anticancer candidates still represents a …
innovation and development of new effective anticancer candidates still represents a …
Dual inhibitors of HDAC and other epigenetic regulators: A novel strategy for cancer treatment
A significant advancement in the field of epigenetic drug discovery has been evidenced in
recent years. Epigenetic alterations are hereditary, nevertheless reversible variations to …
recent years. Epigenetic alterations are hereditary, nevertheless reversible variations to …
Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective
Epigenetic enzymes histone deacetylases (HDACs) are clinically validated anticancer drug
targets which have been studied intensively in the past few decades. Although several drugs …
targets which have been studied intensively in the past few decades. Although several drugs …
Recent updates on thienopyrimidine derivatives as anticancer agents
Thienopyrimidine derivatives hold a unique place between fused pyrimidine compounds.
They are important and widely represented in medicinal chemistry as they are structural …
They are important and widely represented in medicinal chemistry as they are structural …
Two-hit wonders: The expanding universe of multitargeting epigenetic agents
AR De Lera, A Ganesan - Current Opinion in Chemical Biology, 2020 - Elsevier
Multitargeting involves the application of molecules that are deliberately intended to bind to
two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and …
two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and …
Utilization of cyanopyridine in design and synthesis of first-in-class anticancer dual acting PIM-1 kinase/HDAC inhibitors
AKA Bass, ESM Nageeb, MS El-Zoghbi… - Bioorganic …, 2022 - Elsevier
Herein, we report design and synthesis of twenty-one dual PIM-1/HDAC inhibitors utilizing 3-
cyanopyridines as a novel cap moiety linked with aliphatic/aromatic linker bearing carboxylic …
cyanopyridines as a novel cap moiety linked with aliphatic/aromatic linker bearing carboxylic …
Research progress of STAT3-based dual inhibitors for cancer therapy
X Yang, L Xu, L Yang, S Xu - Bioorganic & Medicinal Chemistry, 2023 - Elsevier
Signal transducer and activator of transcription 3 (STAT3), a transcription factor, regulates
gene levels that are associated with cell survival, cell cycle, and immune reaction. It is …
gene levels that are associated with cell survival, cell cycle, and immune reaction. It is …
Design, synthesis, in vitro anticancer evaluation and molecular modelling studies of 3, 4, 5-trimethoxyphenyl-based derivatives as dual EGFR/HDAC hybrid inhibitors
Recently, combining histone deacetylase (HDAC) inhibitors with chemotherapeutic drugs or
agents, in particular epidermal growth factor receptor (EGFR) inhibitors, is considered to be …
agents, in particular epidermal growth factor receptor (EGFR) inhibitors, is considered to be …
[HTML][HTML] HDAC/MIF dual inhibitor inhibits NSCLC cell survival and proliferation by blocking the AKT pathway
Non-small-cell lung carcinoma (NSCLC) is one of the most common forms of lung cancer,
and a leading cause of cancer death among human beings. There is an urgent demand for …
and a leading cause of cancer death among human beings. There is an urgent demand for …