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

• Main Authors: Wei Zhang, Tiantian Sun, Zhenhua Ma, Yingxia Li
• Format: Article
• Language: English
• Published: MDPI AG 2014-04-01
• Series: Marine Drugs
• Subjects: tasiamide; analogues; synthesis; cytotoxicity; marine peptide
• Online Access: http://www.mdpi.com/1660-3397/12/4/2308
• ISSN: 1660-3397

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.