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Marine Spirotetronates: Biosynthetic Edifices That Inspire Drug Discovery

Department of Chemistry & Biochemistry, University of California San Diego, La Jolla, CA 92093-0358, USA
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Mar. Drugs 2019, 17(4), 232; https://doi.org/10.3390/md17040232
Received: 31 March 2019 / Revised: 13 April 2019 / Accepted: 16 April 2019 / Published: 19 April 2019
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. View Full-Text
Keywords: natural product; spirotetronate; antibiotic; anticancer; drug resistance; Diels-Alder; Diels-Alderase; biosynthesis; total synthesis; Bcl-2 inhibitor; pABA inhibitor; UPR apoptosis natural product; spirotetronate; antibiotic; anticancer; drug resistance; Diels-Alder; Diels-Alderase; biosynthesis; total synthesis; Bcl-2 inhibitor; pABA inhibitor; UPR apoptosis
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Braddock, A.A.; Theodorakis, E.A. Marine Spirotetronates: Biosynthetic Edifices That Inspire Drug Discovery. Mar. Drugs 2019, 17, 232.

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