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Phakefustatins A-C: Kynurenine-Bearing Cycloheptapeptides as RXRα Modulators from the Marine Sponge Phakellia fusca.

Ying WuHongze LiaoLi-Yun LiuFan SunHai-Feng ChenHou-Wen LinHong-Rui ZhuFan YangGang HuangDe-Quan ZengMi ZhouShu-Ping WangHou-Wen Lin
Published in: Organic letters (2020)
A neutral-loss scanning mass method was used to explore new kynurenine-containing cycloheptapeptides, phakefustatins A-C (1-3), from the marine sponge Phakellia fusca. Their structures were elucidated by spectroscopic analysis and the advanced Marfey's method. 1 was total synthesized via a final-stage ozonolysis strategy by the combination of solid/solution-phase synthesis. Phakefustatin A (1) was identified as a RXRα modulator to inhibit cancer cell growth, and its pharmacophores could be Kyn and guanidine groups.
Keyphrases
  • high resolution
  • papillary thyroid
  • small molecule
  • molecular docking
  • squamous cell
  • squamous cell carcinoma
  • lymph node metastasis
  • solid state