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Medicinal-Pharmaceutical Chemistry Commons

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Organic Chemistry

2012

Kenneth Lassen

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The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen Feb 2012

The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen

Kenneth Lassen

The tamandarin and didemnins are a class of cyclodepsipeptides that have shown a wide range of biological activity. The didemnins have demonstrated antitumor, antiviral and immunosuppressive activity at low nano- and femtomolar levels. Didemnin B was the first marine natural product to enter clinical trials in humans in the United States. The structures of tamandarins A and B were reported in 2000 and possess almost identical structure and biological activity to didemnin B. These compounds have shown impressive biological activity and some progress has been made in establishing structure-activity relationships. However, their molecular mechanism of action is still unclear. The ...