近年来，含有[1,2,4]噁二唑结构的杂环化合物在生物医药及材料学科得到了迅猛的发展,尤其是它们具有解热镇痛、消炎、降血压、降胆固醇、抗惊厥及抗肿瘤等多种药理活性，且部分噁二唑化合物能够避免多药耐药机制的生成。本项目拟建立以多样性导向合成为策略，采用无溶剂合成、微波辅助合成、“一锅法”合成等简捷高效平行合成[1,2,4]噁二唑类化合物的方法，设计合成一系列结构新颖并具有分子多样性特征的新型[1,2,4]噁二唑类杂环化合物。对所合成的化合物进行体外、体内抗肿瘤活性研究，并通过制备金纳米探针，应用分子生物学手段确认其蛋白作用靶点，筛选出1-2个结构新颖的抗肿瘤药物前体或先导化合物供后续深入研究，这对新型抗肿瘤药物的研发具有较大的科学意义。

In recent years, the heterocyclic compounds containing 1,2,4-oxadiazole skeleton have been developed rapidly in the fields of biomedicine and functional materials. Especially, oxadiazole compounds possess wide spectrum pharmacological activities including antipyretic, analgesic, antiinflammatory, lowering blood pressure, lowering cholesterol, anticonvulsion and antitumor activities, and some of them can avoid the generation mechanism of multidrug resistance. This project will establish a diversity-oriented synthesis strategy, using simple and efficient parallel synthesis methodologies such as solvent-free synthesis, microwave assisted synthesis and "one-pot" synthesis to design and synthesize a series of novel 1,2,4-oxadiazole compounds which possess the characteristics of molecular diversity. Through in vitro and in vivo studies of antitumor activity of the compounds based on gold nano-probe, we intended to apply molecular biology methods to confirm the protein targets of the compounds and finally identify 1-2 antitumor prodrugs or leading compounds for further study. It is of great scientific significance for the research and development of new antitumor drugs.