Department of Chemistry, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Chem Commun (Camb). 2010 Nov 28;46(44):8335-7. doi: 10.1039/c0cc01276a. Epub 2010 Jun 24.
Using click chemistry to enable both structural diversity and proteome profiling within a natural product derived library, two out of nineteen lipstatin analogues showed similar activity to Orlistat against fatty acid synthase (FAS), but with an improved ability to induce tumour cell death.
利用点击化学技术,在天然产物衍生库中实现结构多样性和蛋白质组分析,19 个利普司他汀类似物中有两个表现出与奥利司他类似的脂肪酸合酶(FAS)抑制活性,但诱导肿瘤细胞死亡的能力有所提高。