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Mar. Drugs 2012, 10(12), 2715-2728; doi:10.3390/md10122715

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

1
School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xingang West Road, Guangzhou 510275, China
2
Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China
3
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China
4
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 / Revised: 13 November 2012 / Accepted: 22 November 2012 / Published: 30 November 2012
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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 (222) 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. View Full-Text
Keywords: deoxybostrycin derivatives; antitumor activity; marine mangrove; anthraquinone 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.

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