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

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
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Received: 26 December 2013 / Revised: 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. View Full-Text
Keywords: tasiamide; analogues; synthesis; cytotoxicity; marine peptide tasiamide; analogues; synthesis; cytotoxicity; marine peptide
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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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