design, synthesis and biological evaluation of tasiamide analogues as tumor inhibitors
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ID: 168604
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.
| Reference Key |
zhang2014marinedesign,
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|---|---|
| Authors | ;Wei Zhang;Tiantian Sun;Zhenhua Ma;Yingxia Li |
| Journal | jixie gongcheng xuebao/journal of mechanical engineering |
| Year | 2014 |
| DOI |
10.3390/md12042308
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| URL | |
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