从具有一定生物活性的天然产物中发掘新药资源并试图寻找新药，是新药研究最有效的手段之一。而用多样性导向合成策略建立骨架多样、结构复杂、立体化学多样性的“类天然产物”化合物库进行生物学相关研究、并以此为基础发现药物先导化合物正在成为一种趋势。本研究以我们课题组从木姜子中分离得到的一类新奇骨架类型并有抗HIV活性的Litseane天然倍半萜为研究对象，通过多样性导向合成的策略构建一个类Litseane天然化合物库。设计了一条普适性好，可用来构建结构多样性化合物库的合成路线；并拟合成出100-120个结构新颖的Litseane类天然产物，并对它们的抗HIV活性进行评估及构效关系研究，从中找出影响该类分子的抗HIV活性的结构特征；最终发现活性较好、药用前景广阔的先导化合物。

One of the most effective methods for discovery and development of new drugs is to explore the diversified and biologically active natural products. Employment of diversity-oriented synthesis (DOS), skeleton complex natural product-like libraries can be constructed and used to increase the potential for drug discovery. This strategy will be used in our current study to construct litseane-like library. Litseane belong to sesquiterpenes with a novel skeleton, which were discovered from Litsea verticillata Hance in our research. This class of compounds showed anti-HIV activity. A research object, litseane-like library will be construct by using DOS strategy. A universal synthetic route will be designed and used to synthesize structurally diversified litseanes. We propose to synthesize 100-120 Litseane-like compounds. All of these compound will be new because only 12 litseanes have been reported and 10 of them were discovered in our group. We will further evaluate the anti-HIV activity of the synthesize compounds and interpret their structure-activity relationships. The impact of molecular structural features on their respective anti-HIV activity will be identified. Through this study, we expect to discover litseane lead compounds potent anti-HIV activity and promising pharmaceutical prospect.