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Mar. Drugs 2014, 12(4), 2308-2325; doi:10.3390/md12042308
Article

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

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Received: 26 December 2013; in revised form: 5 March 2014 / Accepted: 18 March 2014 / Published: 22 April 2014
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Abstract: 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.
Keywords: tasiamide; analogues; synthesis; cytotoxicity; marine peptide tasiamide; analogues; synthesis; cytotoxicity; marine peptide
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.

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MDPI and ACS Style

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.

AMA Style

Zhang W, Sun T, Ma Z, Li Y. Design, Synthesis and Biological Evaluation of Tasiamide Analogues as Tumor Inhibitors. Marine Drugs. 2014; 12(4):2308-2325.

Chicago/Turabian Style

Zhang, Wei; Sun, Tiantian; Ma, Zhenhua; Li, Yingxia. 2014. "Design, Synthesis and Biological Evaluation of Tasiamide Analogues as Tumor Inhibitors." Mar. Drugs 12, no. 4: 2308-2325.



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