The Soil Geun-acetic Acid Derivatives Were Designed And Synthesized And Induce Tumor Cell Apoptosis And Antifungal Activity Of Structure-activity Relationship

Tu-Jin-Pi, the root and trunk barks of Pseudolarix kaempferi Gord, has been used in the treatment of dermatological fungal infections in folkloric medicine. Pseudolarix acid B, a compound isolated from the extracts of Tu-Jin-Pi, has been shown to possess significant cytotoxicity for different tumor cell lines and relatively low toxicity. Otherwise, it is active against most of the Candida and Torulopsis species. In our previous work, we have isolated pseudolarix acid B from Tu-Jin-Pi and have synthesized some known hydrolyzed derivatives. In order to find their relationship of structure and activity and to search for drugs with more potent antitumor and antifungi activities, we have synthesized derivatives of Pseudolarix acid B with different ester groups by considering the special structure of pseudolarix acid B and the pharmacological activities of known hydrolyzed derivatives, The derivatives of Pseudolarix acid B were synthesized by cyanuric chloride (CC) . Pharmacological tests showed that most of the derivatives synthesized possessed antitumor and all of the derivatives synthesized possessed antifungi activities in vitro. Based on the experiment results, the relationships of structure and activity are discussed.In this paper, 22 derivatives of Pseudolarix acid B and intermediate 3 are synthesized. 22 derivatives of Pseudolarix acid B are new derivatives identified by IR, ~1H-NMR and MS.