Discovery of novel topoisomerase II inhibitors by medicinal chemistry approaches

W Hu, XS Huang, JF Wu, L Yang… - Journal of Medicinal …, 2018 - ACS Publications
DNA topoisomerase II (topo II) is an important enzyme involved in DNA replication,
recombination, and repair. Despite the popular applications of topo II inhibitors in cancer …

Fused benzo [1, 3] thiazine-1, 2, 3-triazole hybrids: Microwave-assisted one-pot synthesis, in vitro antibacterial, antibiofilm, and in silico ADME studies

ER Sucharitha, TM Krishna, R Manchal… - Bioorganic & Medicinal …, 2021 - Elsevier
In this paper, we report an efficient one-pot three-component reaction sequences comprising
Cu (I)-catalyzed 1, 3-dipolar cycloaddition (CuAAC) followed by Cu-catalyzed arylation of …

Small molecule inhibitors simultaneously targeting cancer metabolism and epigenetics: discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) and …

G Dong, W Chen, X Wang, X Yang, T Xu… - Journal of medicinal …, 2017 - ACS Publications
Cancer metabolism and epigenetics are among the most intensely pursued research areas
in anticancer drug discovery. Here we report the first small molecules that simultaneously …

Evodiamine impairs HIF1A histone lactylation to inhibit Sema3A-mediated angiogenesis and PD-L1 by inducing ferroptosis in prostate cancer

Y Yu, X Huang, C Liang, P Zhang - European Journal of Pharmacology, 2023 - Elsevier
Prostate cancer (PCa) is among the most commonly diagnosed solid cancers in male adults.
However, most anti-angiogenic therapies and immunotherapies fail to achieve durable …

[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 …

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 …

Recent advances in C–H bond functionalization with ruthenium-based catalysts

KS Singh - Catalysts, 2019 - mdpi.com
The past decades have witnessed rapid development in organic synthesis via catalysis,
particularly the reactions through C–H bond functionalization. Transition metals such as Pd …

Design, synthesis and biological evaluation of novel 5, 6, 7-trimethoxy-N-aryl-2-styrylquinolin-4-amines as potential anticancer agents and tubulin polymerization …

S Mirzaei, F Eisvand, F Hadizadeh, F Mosaffa… - Bioorganic …, 2020 - Elsevier
A new series of styrylquinolines was designed and synthesized as anticancer agents and
tubulin polymerization inhibitors. The in vitro anticancer activity of the synthesized quinolines …

Design, synthesis, and evaluation of in vitro and in vivo anticancer activity of 4-substituted coumarins: a novel class of potent tubulin polymerization inhibitors

D Cao, Y Liu, W Yan, C Wang, P Bai… - Journal of medicinal …, 2016 - ACS Publications
In this paper, a series of novel 4-substituted coumarin derivatives were synthesized. Among
these compounds 34, 39, 40, 43, 62, 65, and 67 exhibited significant antiproliferative activity …

An overview on synthetic entries to tetrahydro-β-carbolines

P Maity, D Adhikari, AK Jana - Tetrahedron, 2019 - Elsevier
The tetrahydro-β-carboline (THBC) nucleus is a predominant feature of a vast array of
naturally occurring alkaloids. Most of these alkaloids have been found to exhibit significant …