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Molecules 2014, 19(10), 15572-15583; doi:10.3390/molecules191015572

Development of an Advanced Synthetic Route to Macrosphelides and Its Application to the Discovery of a More Potent Macrosphelide Derivative

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju daero, Jinju 660-701, Gyeongnam, Korea
College of Pharmacy, Seoul National University, Seoul 151-742, Korea
Author to whom correspondence should be addressed.
Received: 12 August 2014 / Revised: 22 September 2014 / Accepted: 24 September 2014 / Published: 29 September 2014
(This article belongs to the Special Issue Heterocyclic and Medicinal Chemistry)
View Full-Text   |   Download PDF [663 KB, uploaded 29 September 2014]   |  


The discovery of a more cytotoxic macrosphelide derivative, including its total synthesis and bioassay are described. Application of the Koide protocol to a readily available propagylic alcohol allowed the rapid and practical synthesis of a macrosphelide A skeleton. This strategy enabled the successful improvement of the cytotoxic activity of the macrosphelide derivative. View Full-Text
Keywords: macrosphelides; natural product; total synthesis macrosphelides; natural product; total synthesis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Heo, Y.M.; Lee, H.; Shin, Y.K.; Paek, S.-M. Development of an Advanced Synthetic Route to Macrosphelides and Its Application to the Discovery of a More Potent Macrosphelide Derivative. Molecules 2014, 19, 15572-15583.

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