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

Marine Drugs

Wei Zhang¹  Tiantian Sun¹  Zhenhua Ma¹ 

[1] Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China;

关键词: tasiamide;    analogues;    synthesis;    cytotoxicity;    marine peptide;   

DOI  :  10.3390/md12042308

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.