Dearomatized xanthone derivatives

Anti-lung cancer activity

A class of highly oxygenated dearomatized novel skeleton molecules from endolichenic fungus, offering a new chemotype for lung cancer therapy.

Wenge, Zhang · Zhu, Lihua · Xu, Ke · Luan, Xiaoyi · Li, Hehe · Zhang, Jiaozhen · Li, Xiuyun · Lou, Hongxiang

Phytochemistry 2026

Specifications

IC50

{'zh': '7.5', 'en': '7.5'} μM

MIC

{'zh': '16', 'en': '16'} μg/mL

Advantages

Clear lung cancer cell inhibition

Compound 9 exhibited moderate inhibitory activity against A549 lung cancer cells with an IC50 of 7.5 μM, serving as a lead for anti-lung cancer optimization.

Antibacterial activity

The MIC against Staphylococcus aureus is 16 μg/mL, suggesting the scaffold may also be developed for antibacterial leads.

Preliminary SAR insight

The conjugated π-system and free phenolic groups are crucial for bioactivity, guiding subsequent structural optimization.

Applications

• Lung cancer targeted therapy：Offers a dearomatized xanthone chemotype that inhibits A549 lung cancer cells.
• Natural product-derived drugs：Novel scaffold from endolichenic fungus, serving as a starting point for natural product-based drug discovery.
• Antitumor lead compounds：Activity and SAR are established, suitable as an antitumor lead for optimization.