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-terminus with 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.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Zhang W,Sun T,Ma Z,Li Ydoi
10.3390/md12042308subject
Has Abstractpub_date
2014-04-22 00:00:00pages
2308-25issue
4issn
1660-3397pii
md12042308journal_volume
12pub_type
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