Tripterygium wilfordii Hook.f. (TWHF^α), commonly known as Lei Gong Teng (Thunder God Vine), is a vine used in traditional Chinese herbal medicine. Triptolide, the major component responsible for the clinical properties of TWHF, is characterized as an abeo-abietane-typed diterpenoid with a unique triepoxide structure and α, β-unsaturated-5-membered lactone. Right after its isolation, triptolide is shown to possess a broad spectrum of pharmacological activities including anticancer, anti-fertility besides its remarkable anti-inflammatory and immunosuppressive activities, which led to extensive studies. Through the modification of different functional groups in triptolide, including the C14-hydroxyl group, C12β, C13β-epoxy group, α, β-unsaturated-5-membered-lactone ring, C7β, C8β-epoxy group, C5, C6-position, and three epoxy ring-opening transformation etc., a series of derivatives are synthesized and their related pharmacological activities are tested. Some preliminary structure-activity relationship (SAR) characteristics are summarized from the pharmacological test results. With the accumulation and deepening of chemical and biological study of 1, its SAR will be clearer. Low toxicity, high activity, and wide therapeutic window derivatives of 1 will definitely make 1 a broad application prospect in many fields.

Contents
1 The structure modification of C14-hydroxyl group
2 The structure modification of C12β,C13β-epoxy group
3 The structure modification of α,β-unsaturated-5-membered-lactone ring
4 The structure modification of C7β,C8β-epoxy group
5 The structure modification on C5,C6-position
6 Structure modification on other sites, or based on various functional groups
7 Introduction of the structure diversity of TWHF diterpenoid derivatives and their structure-activity relationship(SAR)