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Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin
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
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, 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
These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 30 October 2012; in revised form: 13 November 2012 / Accepted: 22 November 2012 / Published: 30 November 2012
Abstract: 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.
Keywords: deoxybostrycin derivatives; antitumor activity; marine mangrove; anthraquinone
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MDPI and ACS Style
Chen, H.; Zhu, X.; Zhong, L.-L.; Yang, B.; Li, J.; Wu, J.-H.; Chen, S.-P.; Lin, Y.-C.; Long, Y.; She, Z.-G. Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin. Mar. Drugs 2012, 10, 2715-2728.
Chen H, Zhu X, Zhong L-L, Yang B, Li J, Wu J-H, Chen S-P, Lin Y-C, Long Y, She Z-G. Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin. Marine Drugs. 2012; 10(12):2715-2728.
Chen, Hong; Zhu, Xun; Zhong, Li-Li; Yang, Bing; Li, Jia; Wu, Jue-Heng; Chen, Sheng-Ping; Lin, Yong-Cheng; Long, Yuhua; She, Zhi-Gang. 2012. "Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin." Mar. Drugs 10, no. 12: 2715-2728.