[HTML][HTML] Evodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity
Y Huang, S Chen, S Wu, G Dong, C Sheng - Acta Pharmaceutica Sinica B, 2020 - Elsevier
A great challenge in multi-targeting drug discovery is to identify drug-like lead compounds
with therapeutic advantages over single target inhibitors and drug combinations. Inspired by …
with therapeutic advantages over single target inhibitors and drug combinations. Inspired by …
Evodiamine-inspired topoisomerase-histone deacetylase dual inhibitors: novel orally active antitumor agents for leukemia therapy
S Wu, Y Huang, T Wang, K Li, J Lu… - Journal of Medicinal …, 2022 - ACS Publications
On the basis of the synergism of topoisomerase (Top) and histone deacetylase (HDAC)
inhibitors in antitumor therapy, a series of novel Top/HDAC dual inhibitors were designed …
inhibitors in antitumor therapy, a series of novel Top/HDAC dual inhibitors were designed …
Design, synthesis, and structure-activity relationships of evodiamine-based topoisomerase (Top)/histone deacetylase (HDAC) dual inhibitors
F Zhu, X Meng, H Liang, C Sheng, G Dong, D Liu… - Bioorganic …, 2022 - Elsevier
On the basis of synergistic effect between topoisomerase (Top) and histone deacetylase
(HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were …
(HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were …
Single inhibitors versus dual inhibitors: role of HDAC in cancer
R Roy, T Ria, D RoyMahaPatra, UH Sk - ACS omega, 2023 - ACS Publications
Due to the multimodal character of cancer, inhibition of two targets simultaneously by a
single molecule is a beneficial and effective approach against cancer. Histone deacetylase …
single molecule is a beneficial and effective approach against cancer. Histone deacetylase …
Multimodal HDAC inhibitors with improved anticancer activity
R Schobert, B Biersack - Current Cancer Drug Targets, 2018 - ingentaconnect.com
Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination
of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat …
of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat …
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer
Z Liang, F Lei, J Deng, H Zhang, Y Wang, J Li… - European journal of …, 2022 - Elsevier
Gastric cancer represents a significant health burden worldwide. Previously, inspired by the
traditional Chinese medicine Wu-Chu-Yu to treat the spleen and stomach system for …
traditional Chinese medicine Wu-Chu-Yu to treat the spleen and stomach system for …
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1, 2, 4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor …
In our study, three series of hydroxamate, 2-aminobenzamide, and trifluoromethyl ketone
analogues have been designed and synthesized. The synthesized compounds were …
analogues have been designed and synthesized. The synthesized compounds were …
Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with antileukemic activity
L Sinatra, J Yang, J Schliehe-Diecks… - Journal of Medicinal …, 2022 - ACS Publications
In this work, we utilized the proteolysis targeting chimera (PROTAC) technology to achieve
the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon …
the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon …
Dual-target inhibitors based on HDACs: novel antitumor agents for cancer therapy
T Liu, Y Wan, Y Xiao, C Xia, G Duan - Journal of medicinal …, 2020 - ACS Publications
Histone deacetylases (HDACs) play an important role in regulating target gene expression.
They have been highlighted as a novel category of anticancer targets, and their inhibition …
They have been highlighted as a novel category of anticancer targets, and their inhibition …
Scaffold diversity inspired by the natural product evodiamine: discovery of highly potent and multitargeting antitumor agents
S Wang, K Fang, G Dong, S Chen, N Liu… - Journal of Medicinal …, 2015 - ACS Publications
A critical question in natural product-based drug discovery is how to translate the product
into drug-like molecules with optimal pharmacological properties. The generation of natural …
into drug-like molecules with optimal pharmacological properties. The generation of natural …
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