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Cyanobacterial Metabolite Calothrixins: Recent Advances in Synthesis and Biological Evaluation

Department of Chemistry, University of Alabama at Birmingham, 901, 14th Street South, Birmingham, AL 35294-1240, USA
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Academic Editor: Paul Long
Mar. Drugs 2016, 14(1), 17; https://doi.org/10.3390/md14010017
Received: 5 August 2015 / Revised: 22 December 2015 / Accepted: 4 January 2016 / Published: 12 January 2016
(This article belongs to the Special Issue Compounds from Cyanobacteria)
The marine environment is host to unparalleled biological and chemical diversity, making it an attractive resource for the discovery of new therapeutics for a plethora of diseases. Compounds that are extracted from cyanobacteria are of special interest due to their unique structural scaffolds and capacity to produce potent pharmaceutical and biotechnological traits. Calothrixins A and B are two cyanobacterial metabolites with a structural assembly of quinoline, quinone, and indole pharmacophores. This review surveys recent advances in the synthesis and evaluation of the biological activities of calothrixins. Due to the low isolation yields from the marine source and the promise this scaffold holds for anticancer and antimicrobial drugs, organic and medicinal chemists around the world have embarked on developing efficient synthetic routes to produce calothrixins. Since the first review appeared in 2009, 11 novel syntheses of calothrixins have been published in the efforts to develop methods that contain fewer steps and higher-yielding reactions. Calothrixins have shown their potential as topoisomerase I poisons for their cytotoxicity in cancer. They have also been observed to target various aspects of RNA synthesis in bacteria. Further investigation into the exact mechanism for their bioactivity is still required for many of its analogs. View Full-Text
Keywords: marine natural product; calothrixin; cyanobacteria; calothrix; antimicrobial activity; anticancer activity; total synthesis marine natural product; calothrixin; cyanobacteria; calothrix; antimicrobial activity; anticancer activity; total synthesis
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MDPI and ACS Style

Xu, S.; Nijampatnam, B.; Dutta, S.; Velu, S.E. Cyanobacterial Metabolite Calothrixins: Recent Advances in Synthesis and Biological Evaluation. Mar. Drugs 2016, 14, 17.

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