Design, synthesis and biological evaluation of tasiamide analogues as tumor inhibitors.

Marine drugs

PubMedID: 24759000

Zhang W, Sun T, Ma Z, Li Y. Design, synthesis and biological evaluation of tasiamide analogues as tumor inhibitors. Mar Drugs. 2014;12(4):2308-25.
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 ┬ÁM 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.