School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xingang West Road, Guangzhou 510275, China.
Mar Drugs. 2012 Nov 30;10(12):2715-28. doi: 10.3390/md10122715.
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.
去氧博斯他汀（1）是一种蒽醌类化合物，来源于海洋红树林真菌 Nigrospora sp. No. 1403，由于其多种生物特性，有可能成为新药的先导化合物。合成了一系列去氧博斯他汀的新衍生物（2-22）。所有新化合物的体外细胞毒性均在 MDA-MB-435、HepG2 和 HCT-116 癌细胞系中进行了测试。大多数化合物表现出较强的细胞毒性，IC₅₀值范围为 0.62 至 10 μM。化合物 19、21 对 MDA-MB-435 的细胞毒性与阳性对照表阿霉素相当。初步筛选结果表明，去氧博斯他汀衍生物可能是新型强效抗癌药物候选物的有价值来源。
