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8 August 2019

Amphidinolides and Iriomoteolides, Potent Anticancer Macrolides †

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Secció de Química Orgànica, Facultat de Química, Universitat de Barcelona, 08028 Barcelona, Spain
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Author to whom correspondence should be addressed.
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
This article belongs to the Proceedings The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery
Amphidinolides and iriomoteolides are complex macrolides isolated from cultured marine dinoflagellates of the genus Amphidinium sp. [1,2,3,4]. All of them are cytotoxic against several cancer cell lines, especially those with larger rings, with activities in the nanomolar range. Some years ago, we started a research program directed towards the synthesis and elucidation of the biological mechanism of action of several members of this family of natural products [5,6,7,8,9]. As part of this research effort, we have completed the total synthesis of some amphidinolides. Work is underway in our laboratories to complete the total synthesis of amphidinolide B2 and iriomoteolide 2a.
Amphidinolide K and some of its stereoisomers and analogues were subjected to evaluation of the possible disruption of the α,β-tubulin–microtubule and/or G-actin–F-actin equilibria. Preliminary studies suggest that amphidinolide K behaves as a stabilizer of F-actin in vitro. The interaction of several of these macrolides with actin has also been studied computationally in our laboratories.

References

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