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

Marine Drugs

Hong Chen¹  Xun Zhu²  Li-Li Zhong¹  Bing Yang¹  Jia Li¹  Jue-Heng Wu²  Sheng-Ping Chen²  Yong-Cheng Lin¹  Yuhua Long³ 

[1] School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xingang West Road, Guangzhou 510275, China;Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China;;School of Chemistry and Environment, South China Normal University, 348 West Outer Ring Road, Guangzhou 510006, China

关键词: deoxybostrycin derivatives;    antitumor activity;    marine mangrove;    anthraquinone;   

DOI  :  10.3390/md10122715

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.