Marine Spirotetronates: Biosynthetic Edifices That Inspire Drug Discovery

Marine Drugs

EmmanuelA. Theodorakis¹  AlexanderA. Braddock² 

[1] Biochemistry, University of California San Diego, La Jolla, CA 92093-0358, USA;;Department of Chemistry &

关键词: natural product;    spirotetronate;    antibiotic;    anticancer;    drug resistance;    Diels-Alder;    Diels-Alderase;    biosynthesis;    total synthesis;    Bcl-2 inhibitor;    pABA inhibitor;    UPR apoptosis;   

DOI  :  10.3390/md17040232

来源: DOAJ

【 摘 要 】

Spirotetronates are actinomyces-derived polyketides that possess complex structures and exhibit potent and unexplored bioactivities. Due to their anticancer and antimicrobial properties, they have potential as drug hits and deserve further study. In particular, abyssomicin C and tetrocarcin A have shown significant promise against antibiotic-resistant S. aureus and tuberculosis, as well as for the treatment of various lymphomas and solid tumors. Improved synthetic routes to these compounds, particularly the class II spirotetronates, are needed to access sufficient quantities for structure optimization and clinical applications.

【 授权许可】

Unknown