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Phakellistatins: An Underwater Unsolved Puzzle

Department of Chemistry and Biology “A. Zambelli”, University of Salerno, Via Giovanni Paolo II, 132-84081 Fisciano (SA), Italy
Department of Organic Chemistry and CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
School of Chemistry and Physics, University of KwaZulu-Natal, Durban 4001, South Africa
Authors to whom correspondence should be addressed.
Mar. Drugs 2017, 15(3), 78;
Received: 10 February 2017 / Revised: 10 March 2017 / Accepted: 15 March 2017 / Published: 18 March 2017
PDF [2203 KB, uploaded 21 March 2017]


A critical summary on the discovery of the nineteen members of the phakellistatin family (phakellistatin 119), cytotoxic proline-rich cyclopeptides of marine origin, is reported. Isolation, structural elucidation, and biological properties of the various-sized natural macrocycles are described, along with the total syntheses and the enigmatic issues of the cytotoxic activity reproducibility. View Full-Text
Keywords: marine sponge; proline-rich cyclopeptide; peptide synthesis; pharmacological activity marine sponge; proline-rich cyclopeptide; peptide synthesis; pharmacological activity

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Meli, A.; Tedesco, C.; Della Sala, G.; Schettini, R.; Albericio, F.; De Riccardis, F.; Izzo, I. Phakellistatins: An Underwater Unsolved Puzzle. Mar. Drugs 2017, 15, 78.

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