The first total synthesis and biological evaluation of marine natural products ma'edamines A and B

作者：Saha Sanjay; Reddy Ch Venkata Ramana; Chiranjeevi T; Addepally Uma; Rao T S Chinta; Patro Balaram^*

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(4): 1013-1016.

DOI：10.1016/j.bmcl.2012.12.033

• Ma'edamine A
• Cytotoxic
• Antiproliferative
• Comet assay
• HER2

We have developed the first total syntheses of marine natural products ma'edamines A (18) and B (20). Structurally, they contain a pyrazine-2-(1H)-one core and were screened for antiproliferative activity on several cancer cell lines. Out of the six cell lines tested, ma'edamines A and B showed significant cytotoxicity against human colon cancer line COLO 205.(IC50 7.9 and 10.3 mu M, respectively), breast cancer cell line MCF-7 (IC50: 6.9 and 10.5 mu M, respectively) and human lung adenocarcinoma cell line A549 (IC50: 12.2 and 15.4 mu M, respectively). The apoptotic effect of ma'edamines was confirmed by comet assay. Hence ma'edamines are likely to be useful as leads for development of a new class of anti-cancer agents.

• 出版日期2013-2-15