Studies on the Synthesis of Derivatives of Marine-Derived Bostrycin and Their Structure-Activity Relationship against Tumor Cells

• Main Authors: Zhigang She, Xun Zhu, Mengfeng Li, Shengping Chen, Yongcheng Lin, Lan Liu, Jia Li, Jueheng Wu, Lili Zhong, Yuhua Long, Hong Chen
• Format: Article
• Language: English
• Published: MDPI AG 2012-04-01
• Series: Marine Drugs
• Subjects: bostrycin; synthesis; antitumor; derivatives; structure-activity relationship
• Online Access: http://www.mdpi.com/1660-3397/10/4/932
• ISSN: 1660-3397

A series of new derivatives (<strong>5</strong>–<strong>29</strong>) of marine-derived bostrycin (<strong>1</strong>) were synthesized. The <em>in vitro</em> cytotoxic activities of all compounds were evaluated against MCF-7, MDA-MB-435, A549, HepG2, HCT-116 and MCF-10A cells using the MTT method. The compounds <strong>7</strong>, <strong>8</strong>, <strong>22</strong>, <strong>23</strong>, <strong>25</strong>, <strong>28</strong> and <strong>29</strong><strong> </strong>of the total showed comparable activity to epirubicin, the positive control, against the tested cancer cell lines. However, these compounds also exhibited cytotoxicity towards MCF-10A cells. The structure-activity relationship (SAR) of bostrycin derivatives was also discussed based on the obtained experimental data.