Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin

• Main Authors: Zhi-Gang She, Yuhua Long, Yong-Cheng Lin, Sheng-Ping Chen, Jue-Heng Wu, Bing Yang, Jia Li, Li-Li Zhong, Hong Chen, Xun Zhu
• Format: Article
• Language: English
• Published: MDPI AG 2012-11-01
• Series: Marine Drugs
• Subjects: deoxybostrycin derivatives; antitumor activity; marine mangrove; anthraquinone
• Online Access: http://www.mdpi.com/1660-3397/10/12/2715
• ISSN: 1660-3397

Deoxybostrycin (1) is an anthraquinone compound derived from the marine mangrove fungus Nigrospora sp. No. 1403 and has potential to be a lead for new drugs because of its various biological properties. A series of new derivatives (2–22) of deoxybostrycin were synthesized. The in vitro cytotoxicity of all the new compounds was tested against MDA-MB-435, HepG2 and HCT-116 cancer cell lines. Most of the compounds exhibit strong cytotoxicity with IC50 values ranging from 0.62 to 10 μM. Compounds 19, 21 display comparable cytotoxicity against MDA-MB-435 to epirubicin, the positive control. The primary screening results indicate that the deoxybostrycin derivatives might be a valuable source of new potent anticancer drug candidates.