ArticleAngewandte Chemie (International ed. in English)2026
Caylobolide B: Structure Revision, Total Synthesis, Biological Characterization, and Discovery of New Analogues.
Article in Angewandte Chemie (International ed. in English), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- Aromatization-Driven Borylene Generation from Borepin Precursors Enables Fused Borirane Synthesis and Selective Alkene Functionalization.Journal of the American Chemical Society · 2026Article
- Canalesolide A, a Structurally Unique Polyhydroxy Macrolide from the Marine Cyanobacterium Okeania sp. with Potent Antitrypanosomal Activity.Journal of the American Chemical Society · 2026Article
- Caylobolide B: Structure Revision, Total Synthesis, Biological Characterization, and Discovery of New Analogues.Angewandte Chemie (International ed. in English) · 2026Article
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Authors and funding
10 authors.
Funding
Abstract
The unique potential of marine polyhydroxylated macrolides in chemical biology and drug discovery has long been constrained by their structural complexity and limited material availability, frustrating efforts in stereochemical assignment, synthesis, and mechanism-of-action elucidation. Here, we establish an integrated workflow, combining chemogenomic profiling, ultra-high-resolution NMR, and modular total synthesis, for the comprehensive functional and structural interrogation of this challenging natural product class. Applying this approach to caylobolides, natural products isolated from scarce samples of Okeania sp., we performed structure-activity relationship studies revealing that acetylation at C29 markedly reduces both cytotoxicity and antifungal activity, pinpointing a key pharmacophore. Mechanistic profiling suggests that these macrolides disrupt membrane integrity, similar to amantelide A. Using natural compound samples, we simultaneously revised the structure of caylobolide B through
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