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Four neoantimycins H-K (1–4) with C1-keto, including the new ones (1–2), were isolated from the culture of  Streptomyces conglobatus  RJ8. After enzymatically converting into their respective reduced type derivatives (5–8)  in vitro , the absolute structures of 1–8 were established/reconfirmed by analyzing hydrolyzed components. The obtained NATs (4, 7, and 8) exhibited excellent cytotoxicity against drug-resistant colon and gastric cancer cells but low toxicity in the noncancerous cell. Further SAR investigation suggested that C1-hydroxyl, C9-isobutyl, and  N -formyl contribute to the antiproliferation remarkably.

Compound Discovery and Structure-Activity Relationship Study of Neoantimycins Against Drug-Resistant Cancer Cells