(199a) Synthesis and Potential Antiproliferative Activity of Dehydroabietylamine Imidazole Derivatives

Xu, L., Nanjing Forestry University
Zhao, F., Nanjing Forestry University
Lu, W., Nanjing Forestry University
Jiang, D., Nanjing Forestry University
Sun, X., Nanjing Forestry University
Yang, S., Nanjing Forestry University
Lin, F., Nanjing Forestry University
Zhou, M., Nanjing Forestry University
Cao, F., Nanjing Forestry University
ABSTRACT: ABSTRACT: Cancer has attracted distinctive attention from all over the world, and extensive research has been devoted to the development of effective anticancer modalities.1-2 Imidazole containing compounds have been found to be very important as anticancer, antimicrobial, antibacterial, antifungal, antioxidant, hypotensive, anti-inflammatory and several important therapeutic agents.3 Recently, a number of bioactive natural products with tricyclic diterpene system have drawn more attention,4 such as dehydroabietylamine (L0). A focus of research of dehydroabietylamine derivatives with their anticancer, antibacterial, antifungal, cytotoxic and antiparasitic activities has attracted wide interest in the forest chemical field. In view of the imidazole and dehydroabietylamine derivatives all have considerable anticancer activities, our group hopes to combine them to synthesize and screen target-specific DNA, high anticancer and low toxic dehydroabietylamine derivatives including organic salts (L1−L2), amides (L3−L5) and Schiff-bases (L6−L7). Among these derivatives, several were designed and synthesized as potent anticancer agents. The antiproliferative activities of these compounds were investigated against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver) human cancer cell lines in vitro by MTT assay. It turned out that many compounds showed high activities against these four cancer cell lines and most of these compounds displayed more potent anticancer activities compared with dehydroabietylamine. Besides, our previous work has tested the inducing-apoptosis ability of the compound L6 and L7. The convenient strategy may be helpful in the development of future generations of anticancer drugs.


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