The Yao Group


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    姚祝军及其研究团队主要研究领域为天然产物的全合成、药物化学和化学生物学,以天然产物全合成为研究手段拓展具有生理活性和药物发展前景的天然与非天然小分子有机化合物,发展分子探针开展相关作用机制的化学生物学研究。代表性成果包括:(1) 完成了cyclomarinchlorofusinchloptosinclavulactonelannotinidine B等复杂生理活性天然产物的首次全合成;(2) 根据“结构展现功能”的指导思想进行类天然产物结构创新,发明了具有细胞选择性的强抗肿瘤活性人工化合物AA005,并通过化学和生物学交叉研究手段基本阐明了AA005 在肿瘤细胞和正常细胞之间产生选择性的特殊机制;(3) 通过合成设计和方法创新相结合,成功建立了路线简短、产率较高的著名生物碱喜树碱和10-羟基喜树碱、抗癌药物伊利替康的对映选择性全合成路线,并发展出活性更强的新颖衍生物;(4) 从经济易得的葡萄糖和氨基酸等原料出发,完成了著名抗流感药物乐感清和达菲的新合成路线;发展并应用多功能有机小分子催化方法,提供了第一条高对映选择性的石杉碱甲催化不对称合成技术路线;(5) 研究了我国中药成分青藤碱的药物化学,发展了一批结构多样的高免疫调节活性青藤碱衍生物。

Fig. Selected bioactive natural products studied and synthesized in this group

        The Yao group mainly focuses on the total synthesis, medicinal chemistry and chemical biology of bioactive natural products. Utilizing innovative synthetic methodologies established in the total syntheses, we are able to develop new chemical entities of medicinal interest and explore the mechanisms of biological action using chemical biology principles. Recent achievements by this group include (1) completion of the first total syntheses of cyclomarin, chlorofusin, chloptosin, clavulactone, lannotinidine B and several other complex bioactive natural products; (2) invention of AA005, an artificial mimicry of cytotoxic acetogenin exhibiting high inhibitory potency against the proliferation of various cancer cells and significant action selectivity between human cancerous and healthy cells, and explanation of the mechanisms associated with the unique cell selectivity; (3) short and high-yielding total syntheses of the famous alkaloids camptothecin (CPT), 10-hydroxycamptothecin and marketed anticancer drug Irinotecan, as well as development of more potent new anticancer derivatives; (4) new economic syntheses of two famous anti-influenza drugs Relenza and Tamiflu from the easily available materials glucono-delta-lactone and amino acids, and the first catalytic asymmetric synthesis of (-)-huperzine A by multifunctional organocatalysis; and (5) development of potent immune-regulating agents from economically available alkaloid sinomenine, a poorly active TCM intergradient.

 
 

Office E515, Lab B505 511 512, School of Chemistry and Chemical Engineering,
State Key Laboratory of Coordination Chemistry and Nanjing National Laboratory of Microstructures,  Nanjing University, 163 Xianlin Avenue Nanjing, Jiangsu, China
Tel: +86-25-89683732 E-mail: yaoz@nju.edu.cn
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