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

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...

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Bibliographic Details
Published in:Marine drugs 2014-04, Vol.12 (4), p.2308-2325
Main Authors: Zhang, Wei, Sun, Tiantian, Ma, Zhenhua, Li, Yingxia
Format: Article
Language:English
Subjects:
analogues
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Carcinoma
Carcinoma, Non-Small-Cell Lung - drug therapy
Carcinoma, Non-Small-Cell Lung - pathology
Cell Line, Tumor
cytotoxicity
Humans
Inhibitory Concentration 50
Lung Neoplasms - drug therapy
Lung Neoplasms - pathology
Marine
marine peptide
Nasopharyngeal Carcinoma
Nasopharyngeal Neoplasms - drug therapy
Nasopharyngeal Neoplasms - pathology
Oligopeptides - chemical synthesis
Oligopeptides - chemistry
Oligopeptides - pharmacology
Structure-Activity Relationship
synthesis
tasiamide
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Summary: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.
ISSN:1660-3397
1660-3397
DOI:10.3390/md12042308