Precursor-Directed Biosynthesis of Neoantimycin Derivatives with Selective Cytotoxicity.

J Nat Prod

Institute of Marine Drugs, Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, People's Republic of China.

Published: May 2024

A precursor-directed biosynthesis approach led to the accumulation of seven new neoantimycin derivatives (-) from RJ2. Structure elucidation was conducted using NMR and HRESIMS analysis, and the absolute configuration was determined by advanced Marfey's method, Mosher's analysis, and ECD analysis. The obtained compounds revealed selective and significant cytotoxicity, specifically against colorectal cancer cells bearing the K-ras mutation, with IC values ranging from 40 nM to 3.5 μM.

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http://dx.doi.org/10.1021/acs.jnatprod.4c00013DOI Listing

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