Chalcone derivatives: role in anticancer therapy

Y Ouyang, J Li, X Chen, X Fu, S Sun, Q Wu - Biomolecules, 2021 - mdpi.com
Chalcones (1, 3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids,
which are common simple chemical scaffolds found in many naturally occurring compounds …

Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer

AA WalyEldeen, S Sabet, HM El-Shorbagy… - Chemico-Biological …, 2023 - Elsevier
The need for innovative anticancer treatments with high effectiveness and low toxicity is
urgent due to the development of malignancies that are resistant to chemotherapeutic …

A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

W Liu, M He, Y Li, Z Peng, G Wang - Journal of enzyme inhibition …, 2022 - Taylor & Francis
Microtubules play an important role in the process of cell mitosis and can form a spindle in
the mitotic prophase of the cell, which can pull chromosomes to the ends of the cell and then …

Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer …

MAE Mourad, A Abo Elmaaty, I Zaki… - Journal of Enzyme …, 2023 - Taylor & Francis
Topoisomerases II are ubiquitous enzymes with significant genotoxic effects in many critical
DNA processes. Additionally, epidermal growth factor receptor (EGFR) plays pivotal role in …

Efficient synthesis and bioevaluation of novel dual tubulin/histone deacetylase 3 inhibitors as potential anticancer agents

X Peng, J Chen, L Li, Z Sun, J Liu, Y Ren… - Journal of Medicinal …, 2021 - ACS Publications
Novel dual HDAC3/tubulin inhibitors were designed and efficiently synthesized by
combining the pharmacophores of SMART (tubulin inhibitor) and MS-275 (HDAC inhibitor) …

From natural products to HDAC inhibitors: An overview of drug discovery and design strategy

X Qiu, L Zhu, H Wang, Y Tan, Z Yang, L Yang… - Bioorganic & Medicinal …, 2021 - Elsevier
Histone deacetylases (HDACs) play a key role in the homeostasis of protein acetylation in
histones and have recently emerged as a therapeutic target for numerous diseases. The …

Design, synthesis, cytotoxic activities, and molecular docking of chalcone hybrids bearing 8-hydroxyquinoline moiety with dual tubulin/EGFR kinase inhibition

MM Amin, GEDA Abuo-Rahma, MSA Shaykoon… - Bioorganic …, 2023 - Elsevier
The present study established thirteen novel 8-hydroxyquinoline/chalcone hybrids 3a–m of
hopeful anticancer activity. According to NCI screening and MTT assay results, compounds …

Identification of novel leads as potent inhibitors of HDAC3 using ligand-based pharmacophore modeling and MD simulation

N Kumbhar, S Nimal, S Barale, S Kamble, R Bavi… - Scientific Reports, 2022 - nature.com
In the landscape of epigenetic regulation, histone deacetylase 3 (HDAC3) has emerged as a
prominent therapeutic target for the design and development of candidate drugs against …

Discovery of a novel vascular disrupting agent inhibiting tubulin polymerization and HDACs with potent antitumor effects

H Zhu, Y Tan, C He, Y Liu, Y Duan, W Zhu… - Journal of medicinal …, 2022 - ACS Publications
Most vascular disrupting agents (VDAs) fail to prevent the regrowth of blood vessels at the
edge of tumors, causing tumor rebound and relapse. Herein, a series of novel …

Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency

Y Wang, M Sun, Y Wang, J Qin, Y Zhang… - European Journal of …, 2021 - Elsevier
A novel series of cis-diphenylethene and benzophenone derivatives as tubulin/HDAC dual-
targeting inhibitors were designed and synthesized. Among them, compound 28g exhibited …