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 …

Scaffold hopping of natural product evodiamine: discovery of a novel antitumor scaffold with excellent potency against colon cancer

L Wang, K Fang, J Cheng, Y Li, Y Huang… - Journal of Medicinal …, 2019 - ACS Publications
Inspired by the natural product evodiamine, a novel antitumor indolopyrazinoquinazolinone
scaffold was designed by scaffold hopping. Structure–activity relationship studies led to the …

New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure–activity relationship analysis …

G Dong, S Wang, Z Miao, J Yao, Y Zhang… - Journal of medicinal …, 2012 - ACS Publications
Evodiamine is a quinazolinocarboline alkaloid isolated from the fruits of traditional Chinese
herb Evodiae fructus. Previously, we identified N13-substituted evodiamine derivatives as …

Natural product evodiamine-inspired medicinal chemistry: Anticancer activity, structural optimization and structure-activity relationship

Z Wang, Y Xiong, Y Peng, X Zhang, S Li, Y Peng… - European Journal of …, 2023 - Elsevier
It is a well-known phenomenon that natural products can serve as powerful drug leads to
generate new molecular entities with novel therapeutic utility. Evodiamine (Evo), a major …

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 …

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 …

Selection of evodiamine as a novel topoisomerase I inhibitor by structure-based virtual screening and hit optimization of evodiamine derivatives as antitumor agents

G Dong, C Sheng, S Wang, Z Miao, J Yao… - Journal of medicinal …, 2010 - ACS Publications
Human topoisomerase I (TopoI) is recognized as a valuable target for the development of
effective antitumor agents. Structure-based virtual screening was applied to the discovery of …

[HTML][HTML] PROTAC derivatization of natural products for target identification and drug discovery: Design of evodiamine-based PROTACs as novel REXO4 degraders

S Chen, K Bi, H Liang, Z Wu, M Huang, X Chen… - Journal of advanced …, 2023 - Elsevier
Abstract Introduction Natural products (NPs) play a crucial role in the development of
therapeutic drugs. However, it is still highly challenging to identify the targets of NPs …

Evodiamine as an anticancer agent: a comprehensive review on its therapeutic application, pharmacokinetic, toxicity, and metabolism in various cancers

M Panda, SK Tripathi, G Zengin, BK Biswal - Cell Biology and Toxicology, 2023 - Springer
Evodiamine is a major alkaloid component found in the fruit of Evodia rutaecarpa. It shows
the anti-proliferative potential against a wide range of cancers by suppressing cell growth …

Improved total synthesis of tubulysins and design, synthesis, and biological evaluation of new tubulysins with highly potent cytotoxicities against cancer cells as …

KC Nicolaou, RD Erande, J Yin… - Journal of the …, 2018 - ACS Publications
Improved, streamlined total syntheses of natural tubulysins such as V (Tb45) and U (Tb46)
and pretubulysin D (PTb-D43), and their application to the synthesis of designed tubulysin …