Design and Synthesis of Novel Caudatin Derivatives Containing Arylacryloyl and Quinolyl Substituents With Anticancer Activity
Open Access
- 15 October 2026
- journal article
- research article
- Published by Wiley in Chemistry & Biodiversity
- Vol. 23 (10) , e71821
Abstract
Caudatin ( 1 ) represents one of major C 21 ‐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 IC 50 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.Keywords
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