Synthesis Of Pseudolaric Acid B Derivatives And Its Antitumor Activity

During the past ten years,more attentions have been given to uncovering the benefits of the natural products in relation to cancers. Pseudolaric acid B (PB), a novel diterpene acid, isolated from Pseudolarix kaempferi Gorden and identified as the main antifungal constituent, possesses various pharmacological activities. Recently, PB has been noted for its notable cytotoxic activity against P-388 lymphocytic leukemia, KB carcinoma of the nasopharynx, HT-1080 fibrosarcom, human breast cancer, human melanoma, human lung cancer and human colon cancer cell lines in vitro.Objective: Synthesis a series of derivatives of Pseudolaric acid B at the conjugated diene acid side chain and methyl ester part respectively, testing its antitumor activity to different tumor cell lines in vitro, evaluating the groups necessary for antitumor activity and the structure-activity relationship(SAR) of Pseudolaric acid B, synthesizing some new compounds with high antitumor activity.Methods: 1. The isolation of Pseudolaric acid B: crushed pseudolarix soaked in 95% alcohol 8 times in volume than the raw material in weight, combining the extract after refluxed...