[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 …

Design, synthesis, and evaluation of chalcone analogues incorporate α, β-Unsaturated ketone functionality as anti-lung cancer agents via evoking ROS to induce …

M Zhu, J Wang, J Xie, L Chen, X Wei, X Jiang… - European Journal of …, 2018 - Elsevier
Chalcone, a natural structure, demonstrates many pharmacological activities including
anticancer, and one promising mechanism is to modulate the generation of ROS. It has been …

Design, synthesis and bioactivity study of evodiamine derivatives as multifunctional agents for the treatment of hepatocellular carcinoma

X Fan, J Deng, T Shi, H Wen, J Li, Z Liang, F Lei… - Bioorganic …, 2021 - Elsevier
Topoisomerase has been found extremely high level of expression in hepatocellular
carcinoma (HCC) and proven to promote the proliferation and survival of HCC. Cancer …

[HTML][HTML] Novel fluorescent probes of 10-hydroxyevodiamine: autophagy and apoptosis-inducing anticancer mechanisms

S Chen, G Dong, S Wu, N Liu, W Zhang… - … Pharmaceutica Sinica B, 2019 - Elsevier
Natural product evodiamine and its derivatives represent a promising class of multi-target
antitumor agents. However, the clinical development of these compounds has been …

Discovery of novel polycyclic heterocyclic derivatives from evodiamine for the potential treatment of triple-negative breast cancer

S Xu, H Yao, Y Qiu, M Zhou, D Li, L Wu… - Journal of Medicinal …, 2021 - ACS Publications
Evodiamine (Evo) is a quinazolinocarboline alkaloid found in Evodia rutaecarpa and
exhibits moderate antiproliferative activity. Herein, we report using a scaffold-hopping …

Discovery of evodiamine derivatives as highly selective PDE5 inhibitors targeting a unique allosteric pocket

T Zhang, Z Lai, S Yuan, YY Huang… - Journal of medicinal …, 2020 - ACS Publications
Clinical use of phosphodiesterase-5 (PDE5) inhibitors is limited by several side effects due
to weak isoform selectivity. Herein, a unique allosteric pocket of PDE5 is identified by …

Mild and General Synthesis of Pyrrolo[2,1-a]isoquinolines and Related Polyheterocyclic Frameworks from Pyrrole Precursors Derived from a Mechanochemical …

M Leonardi, M Villacampa… - The Journal of Organic …, 2017 - ACS Publications
The combination of a three-component, solvent-free pyrrole synthesis performed under
mechanochemical conditions with a TMSOTf-catalyzed oxonium-mediated cyclization gave …

Structure-based design and synthesis of N-substituted 3-amino-β-carboline derivatives as potent αβ-tubulin degradation agents

Y Li, Y Liu, Z Zhu, W Yan, C Zhang… - Journal of Medicinal …, 2022 - ACS Publications
So far, relatively few small molecules have been reported to promote tubulin degradation.
Our previous studies have found that compound 2, a noncovalent colchicine-site ligand, was …

[HTML][HTML] Evodiamine attenuates experimental colitis injury via activating autophagy and inhibiting NLRP3 inflammasome assembly

W Ding, Z Ding, Y Wang, Y Zhu, Q Gao… - Frontiers in …, 2020 - frontiersin.org
Autophagy and NLRP3 inflammasome were associated with the process of colitis. Drugs
targeting NLRP3 inflammasome and autophagy to treat colitis are absent, and they are …

1 (3)‐Formyl‐β‐carbolines: Potential Aldo‐X Precursors for the Synthesis of β‐Carboline‐Based Molecular Architectures

N Devi, S Kumar, SK Pandey… - Asian Journal of Organic …, 2018 - Wiley Online Library
Abstract β‐Carboline, a privileged scaffold in the alkaloid family, has a broad spectrum of
medicinal properties and is found in several commercial drugs, such as tadalafil …