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.
Highlights
Mortality and morbidity of cancer patients is the second highest among all diseases in the world, following heart disease [1–3]
Deoxybostrycin reacted with 2,2-dimethoxypropane and polyoxymethylene in the presence of 1 equivalent of p-toluenesulfonic acid (TsOH) at room temperature to give 2,3-ketal derivatives 2 and
When deoxybostrycin reacted with various amines at room temperature using methanol as solvent, a series of alkylamino and arylamino derivatives 4–17 were obtained (Scheme 2)
Summary
Mortality and morbidity of cancer patients is the second highest among all diseases in the world, following heart disease [1–3]. Due to drawbacks of chemotherapy, such as dose limits, side effects, and low selectivity to cancer cells, discovery and development of much more effective, safe and highly selective antitumor drugs is still an urgent task. Recent reviews of drug discovery literature have shown that more than two thirds of the anticancer drugs approved between the 1940s and 2006 are either natural products or developed based on the knowledge gained from natural products [4,5]. Marine microorganisms have attracted great attention in the pharmaceutical community as they produce a wide variety of metabolites that are structurally unique and pharmacologically active [6,7]. Due to the structural and bioactive diversities of marine microorganism metabolites, they represent a promising resource for discovering new anticancer drugs [8,9]
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