Eskitis Institute, Griffith University, Nathan, QLD 4111, Australia.
Org Biomol Chem. 2011 Jun 21;9(12):4570-9. doi: 10.1039/c1ob05299c. Epub 2011 May 3.
A novel harringtonolide-inspired scaffold containing a cycloheptatriene ring and two fused cyclopentane rings has been synthesised from simple starting materials. The scaffold, containing a similar substitution pattern and relative stereochemistry to the complex diterpenoid, has been enumerated into a small library of derivatives. One of these library members has been converted into a sub-library of substituted triazoles using copper-catalysed azide-alkyne cycloaddition (click) chemistry. The scaffold may be useful in drug discovery or in the preparation of additional molecular probes for chemical biology.
一种新型的哈林通内酯骨架，包含一个环己三烯环和两个融合的环戊烷环，已经从简单的起始原料中合成。该支架包含与复杂二萜类似的取代模式和相对立体化学，已被枚举为一个小型衍生物文库。这些文库成员之一已通过铜催化的叠氮化物-炔烃环加成（点击）化学转化为取代三唑的子文库。该支架可能在药物发现或为化学生物学制备其他分子探针方面有用。
