Synthesis and biological evaluation of (+)-neopeltolide analogues: Importance of the oxazole-containing side chain

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• 作者：Haruhiko Fuwa ; ^{hfuwa@m.tohoku.ac.jp" class="auth_mail} ; Takuma Noguchi ; Masato Kawakami ; Makoto Sasaki
• 关键词：Marine natural products ; Macrolides ; Antiproliferative activity ; Structure&ndash ; activity relationships ; Suzuki&ndash ; Miyaura coupling
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 June 2014
• 年：2014
• 卷：24
• 期：11
• 页码：2415-2419
• 全文大小：1079 K

文摘

We describe the synthesis and biological evaluation of (+)-neopeltolide analogues with structural modifications in the oxazole-containing side chain. Evaluation of the antiproliferative activity of newly synthesized analogues against A549 human lung adenocarcinoma cells and PANC-1 human pancreatic carcinoma cells have shown that the C19–C20 and C26–C27 double bonds within the oxazole-containing side chain and the terminal methyl carbamate group are essential for potent activity.