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Synthesis and Anti-tumor Activities of a Novel Class of Dehydroabietylamine Derivatives

机译:一种新型脱氢表达衍生物的合成与抗肿瘤活性

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Structural modification is still a popular and important route in the forest chemical field for finding novel dehydroabietylamine derivatives with more potential bioactivities and broad bioactive spectra. In this work, a series of dehydroabietylamine derivatives containing tricyclic diterpene structure were synthesized through oxidation in the 7 position of ring B and nitrification in the 12 position of ring C using dehydroabietylamine as raw materials. Chromium trioxide-acetic acid was used as oxidizing reagent and copper nitrate-acetic anhydride was used as nitrating reagent in the synthetic process. Structures of the synthesized compounds were confirmed by IR, NMR and MS. The cytotoxicity of these compounds against PC-3(human prostate carcinoma cell line) and Hey-1B(human ovarian carcinoma cell line) cancer cells by MTT assay were investigated. The results demonstrated that some of the synthesized compounds exhibited somewhat antitumor activities. The information obtained from this study may be useful for the design of novel chemotherapeutic drugs. Additional pharmacology research work is still in progress.
机译:结构改性仍然是森林化学领域的流行和重要的路线,用于寻找具有更多潜在的生物活性和广泛的生物活性光谱的新型脱氢表达胺衍生物。在这项工作中,通过氧化在环B的7个位置中的氧化和环C的12个位置,使用脱氢表达胺作为原料,通过氧化合成一系列含有三环二萜结构的脱氢表达衍生物。三氧化铬 - 乙酸用作氧化试剂,硝酸铜 - 乙酸铜用作合成方法中的硝化试剂。通过IR,NMR和MS确认合成化合物的结构。通过MTT测定研究了这些化合物对PC-3(人前列腺癌细胞系)和HEY-1B(人卵巢癌细胞系)癌细胞的细胞毒性。结果表明,一些合成的化合物表现出稍微抗肿瘤活性。本研究中获得的信息可用于设计新型化学治疗药物。额外的药理学研究工作仍在进行中。

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