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Design and Synthesis of Novel Caudatin Derivatives Containing Arylacryloyl and Quinolyl Substituents With Anticancer Activity.

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Τίτλος: Design and Synthesis of Novel Caudatin Derivatives Containing Arylacryloyl and Quinolyl Substituents With Anticancer Activity.
Συγγραφείς: Li XS; Guangdong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, PR China., Zhan HH; Guangdong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, PR China.; Guangdong (Zhanjiang) Provincial Laboratory of Southern Marine Science and Engineering, Zhanjiang, PR China., Wang XH; Guangdong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, PR China.; School of Pharmacy, Guangdong Medical University, Dongguan, PR China., Zheng TX; Guangdong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, PR China., Li BB; School of Pharmacy, Guangdong Medical University, Dongguan, PR China., Chen HT; School of Pharmacy, Guangdong Medical University, Dongguan, PR China., Su AY; The First School of Clinical Medicine, Guangdong Medical University, Zhanjiang, PR China., Liu L; School of Pharmacy, Guangdong Medical University, Dongguan, PR China., Yang XM; School of Pharmacy, Guangdong Medical University, Dongguan, PR China., Luo H; Guangdong Engineering Technology Research Center for the Development and Utilization of Mangrove Wetland Medicinal Resources, School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang, PR China.; Guangdong (Zhanjiang) Provincial Laboratory of Southern Marine Science and Engineering, Zhanjiang, PR China.
Πηγή: Chemistry & biodiversity [Chem Biodivers] 2026 Oct; Vol. 23 (10), pp. e71821.
Τύπος έκδοσης: Journal Article
Γλώσσα: English
Στοιχεία περιοδικού: Publisher: Verlag Helvetica Chimica Acta Country of Publication: Switzerland NLM ID: 101197449 Publication Model: Print Cited Medium: Internet ISSN: 1612-1880 (Electronic) Linking ISSN: 16121872 NLM ISO Abbreviation: Chem Biodivers Subsets: MEDLINE
Imprint Name(s): Original Publication: Zürich, Switzerland : Hoboken, NJ : Verlag Helvetica Chimica Acta ; Distributed in the USA by Wiley, c2004-
Ιατρικοί όροι (MeSH): Steroids*/chemistry , Steroids*/chemical synthesis , Steroids*/pharmacology , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Saponins*/chemistry , Saponins*/chemical synthesis , Saponins*/pharmacology , Antineoplastic Agents, Phytogenic*/pharmacology , Antineoplastic Agents, Phytogenic*/chemistry , Antineoplastic Agents, Phytogenic*/chemical synthesis , Drug Design*, Apoptosis/drug effects ; Cell Proliferation/drug effects ; Cynanchum/chemistry ; Cell Cycle/drug effects ; Humans ; Structure-Activity Relationship ; Drug Screening Assays, Antitumor ; Cell Line, Tumor ; Molecular Structure ; Glycosides
Περίληψη: Caudatin (1) represents one of major C21-steroids isolated from Cynanchum otophyllum. Thirty-one novel caudatin derivatives with arylacryloyl (1a-1w) and quinolyl (2a-2h) substituents were synthesized and structurally characterized by spectroscopic analysis. Their anticancer activities were evaluated against four human cancer cell lines (MCF-7, H1299, HeLa, and HepG2). Most compounds exhibit significant antiproliferative effects, among which 1b and 2h demonstrated broad-spectrum activity with IC50 values of 8.54-12.12 and 11.43-14.25 uM, respectively. Further mechanistic studies showed that 1b induced marked apoptosis in HepG2 cells and modulated cell cycle distribution, with a higher percentage of cells accumulating in the G0/G1 phase at increased concentrations. Overall, these findings indicate that caudatin derivatives bearing arylacryloyl and quinolyl moieties constitute a preliminary chemical framework for the development of antitumor candidates for caudatin-like natural products.
(© 2026 The Author(s). Chemistry & Biodiversity published by Wiley‐VHCA AG.)
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Grant Information: GDNRC [2022]38 Economic Development of Marine Economy of Guangdong Province, China; GDMUZDCG25020 Guangdong Medical University; GDMUZDCG25023 Guangdong Medical University; JDXM2024094 Undergraduate Innovation and Entrepreneurship Education Base Project of Guangdong Medical University; JDXM2025049 Undergraduate Innovation and Entrepreneurship Education Base Project of Guangdong Medical University; JDXM2025086 Undergraduate Innovation and Entrepreneurship Education Base Project of Guangdong Medical University; JDXM2025124 Undergraduate Innovation and Entrepreneurship Education Base Project of Guangdong Medical University; JDXM2025189 Undergraduate Innovation and Entrepreneurship Education Base Project of Guangdong Medical University
Contributed Indexing: Keywords: anticancer activity; arylacryloyl and quinolyl substituents; caudatin; synthesis
Substance Nomenclature: 0 (Steroids)
0 (caudatin)
0 (Antineoplastic Agents)
0 (Saponins)
0 (Antineoplastic Agents, Phytogenic)
0 (Glycosides)
Entry Date(s): Date Created: 20261015 Date Completed: 20261015 Latest Revision: 20261017
Update Code: 20261017
PubMed Central ID: PMC13670407
DOI: 10.1002/cbdv.71821
PMID: 42878227
Βάση Δεδομένων: MEDLINE
Περιγραφή
ISSN:1612-1880
DOI:10.1002/cbdv.71821