Design, Synthesis And Biological Activity Of Xanthone Derivatives

In search for biological activity lead compounds and development of new drugs from natural products still is recognized as one of the effective ways. To modificate the known structure of the natural products or drugs is a important way in new drug research. Xanthone derivatives with oxygenated heterocyclic compounds are widely distributed in plants and microorganisms. They have a broad spectrum of biological activities, such as antioxidative, antitumor, antifungal and antidiabetic. In this paper, forty xanthone derivatives were designed and synthesized by introducing different pharmacophores to the xanthone scaffold. All of them were reported firstly and the structures were determined by1H NMR. At the same time their pharmacological activities are being evaluated as antitumor.The malignant tumor is a highly prevalent disease that poses an increasing public health threat worldwide. It is reported that xanthone could act efficient DNA intercalators and topoisomerase inhibitors, displaying interesting anticancer activity. On the other hand,1,2,3-triazoles are favorite groups in various fields of drug design. Especially, their potent antitumor effect gains our great interest.According to the combination principles in drug design, two series of novel xanthone derivatives containing1,2,3--triazole and benzyl were designed and synthesized.The xanthone frameworks were achieved by using F-C acylation and cyclization, which were gotten propargylation in1-OH by reacting with propargyl bromide."Click reaction" was successfully employed for the synthesis of the designed target compounds. The reaction of corresponding benzylbromide with sodium azide and terminal alkynes yielded target compounds in the presence of Na-ascorbate(5mol%) and CuSO4·5H2O(1mol%) with high yield.All the prepared compounds were screened for their activities against human hepatoma carcinoma cell line and cervical carcinoma cell line using the MTT colorimetric method.