Naphthacemycins from a <i>Streptomyces</i> sp. as Protein-Tyrosine Phosphatase Inhibitors
Changhong Huo, Zhihui Zheng, Yan Xu, Yanbo Ding, Haizhou Zheng, Yunlong Mu, Yuanchen Niu, Jian Gao, Xinhua Lu
Abstract
Nine new naphthacemycins (1–9), along with one known naphthacemycin (10) were isolated from the culture of Streptomyces sp. N12W1565. Their structures were elucidated on the basis of spectroscopic analysis, including UV, NMR, and HRESIMS. All the compounds showed significant activity, with IC50 values less than 10 μM against protein-tyrosine phosphatase 1B (PTP1B). The anti-PTP1B structure–activity relationship of naphthacemycins (1–10) is discussed. These findings provide a promising starting point for the development of naphthacemycins as potential anti-PTP1B agents.
Topics & Concepts
StreptomycesProtein tyrosine phosphataseStreptomycetaceaePhosphataseBiochemistryBiologyActinomycetalesStereochemistryTyrosineChemistryMicrobiologyEnzymeBotanyBacteriaGeneticsProtein Tyrosine PhosphatasesBiochemical and Molecular ResearchBioactive Compounds and Antitumor Agents