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Mar. Drugs 2014, 12(4), 2308-2325;

Design, Synthesis and Biological Evaluation of Tasiamide Analogues as Tumor Inhibitors

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China
Author to whom correspondence should be addressed.
Received: 26 December 2013 / Revised: 5 March 2014 / Accepted: 18 March 2014 / Published: 22 April 2014
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Eighteen analogues of the marine cytotoxic linear peptide tasiamide were designed, synthesized and screened for their inhibitory activities against the growth of human nasopharyngeal carcinoma (KB) and human non-small cell lung tumor (A549) cell lines. The results indicated that minor modifications of the C-terminuswith aromatic groups were tolerated, with the IC50 values between 1.29 and 12.88 μM against these two cancer cell lines. Truncation, minor modifications at the N-terminus or elimination of the N-methyl groups in N-Me-d-Gln and/or N-Me-d-Phe residues resulted in inactive analogues. View Full-Text
Keywords: tasiamide; analogues; synthesis; cytotoxicity; marine peptide tasiamide; analogues; synthesis; cytotoxicity; marine peptide

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Zhang, W.; Sun, T.; Ma, Z.; Li, Y. Design, Synthesis and Biological Evaluation of Tasiamide Analogues as Tumor Inhibitors. Mar. Drugs 2014, 12, 2308-2325.

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