ArticleDrug development research2025
Novel Oxadiazole-Based Bioisostere of Caffeic Acid Phenethyl Ester: Synthesis, Anticancer Activity, and Inhibition of Lipoxygenase Product Biosynthesis.
Article in Drug development research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Recent Developments in Ferulic Acid- and Caffeic Acid-Based Hybrids with Potential Anticancer Properties.Molecules (Basel, Switzerland) · 2026Review
- Targeting in vitro vasculogenic mimicry and associated stemness transcriptional signature in human ovarian cancer cell models: new emerging roles of caffeic acid phenethyl ester synthetic analogs.Frontiers in pharmacology · 2026Article
Corrections and comments
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Authors and funding
6 authors.
Funding
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Abstract
Caffeic acid phenethyl ester (1), a honeybee propolis component, possesses many bioactive properties, making it a useful scaffold for drug research. Further, CAPE (1) is a more effective inhibitor of the biosynthesis of 5-lipoxygenase (5-LO) products compared to Zileuton, the only clinically-approved direct 5-LO inhibitor. However, CAPE (1) suffers from a poor metabolic profile, being rapidly metabolized to caffeic acid (CA). In this study, we synthesized and performed several biological assays on a new bioisostere of CAPE (1) possessing a 1,2,4-oxadiazole ring. The new bioisostere (OB-CAPE (5)) has a similar antiproliferative effect to CAPE (1) on NCI-60 cancer cell lines and maintains the activity of CAPE (1) as an inhibitor of the biosynthesis of 5-, 12- and 15-LO products and as an iron chelator. In human polymorphonuclear leukocytes, OB-CAPE (5) inhibits the biosynthesis of 5-LO products with an IC
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