Caylobolide B: Structure Revision, Total Synthesis, Biological Characterization, and Discovery of New Analogues.

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 pharmac

SUBMITTER: George MRP 

PROVIDER: S-EPMC12828451 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature