From trees to treatments. Catalytic amination of terpenes and biological screening

BC的森林产品富含天然存在的萜烯，这是一类具有抗真菌，抗细菌和药用生物活性的分子。这些分子可以进一步进行化学修饰，以获得具有商业价值的化合物，如香料和芳香剂，以及药物，除草剂和杀虫剂。所有这些产品都是生物产品，它们增加了BC省林业产业的商业机会。值得注意的是，萜烯的化学修饰还没有包括将氮引入这些复杂分子结构的策略。然而，含氮的萜烯类化合物是一类天然产物，被称为萜类生物碱，这类天然产物显示出强大的生物活性。例如，萜类生物碱已被用于癌症治疗和心脏病治疗。UBC的Schafer实验室最近的进展导致了新的催化技术的发展，该技术可以在一个有效的化学转化中将氮安装到萜烯中。没有废物的副产品形成和转换是能源效率，使这种化学反应理想地适用于在商业过程中的应用。该提案将制备20种不同的合成萜类生物碱作为潜在药物进行研究。这项工作将与纳奈莫森林产品公司合作完成，以确定用于修饰的首选萜烯，并与温哥华的药物研究和开发中心合作，筛选具有生物活性的新萜类生物碱。

BC's forest products are rich in naturally occuring terpenes, a class of molecules that display anti-fungal,anti-bacterial and medicinal bioactivity. These molecules can be further chemically modifed to accesscompounds of commercial value as flavours and fragrances as well as medicines, herbicides and pesticides.All of these products are bioproducts and they enhance the commercial opportunity of BC's Forestry Industry.Notably chemical modification of terpenes has not included strategies for incorporating nitrogen into thesecomplex molecular structures. However, nitrogen containing terpenes are a class of naturally occuringproducts called terpenoid-alkaloids and such natural products are known to display potent biological activity.For example, terpenoid-alkaloids have been used in cancer therapies and in treatments for heart disease.Recent advances in the Schafer laboratory at UBC have resulted in the development of new catalytictechnologies that can install nitrogen into terpenes in one efficient chemical transformation. There are nowaste by-products formed and the transformation is energy efficient, making this chemical reaction ideallysuited for application in commercial processes. This proposal will prepare 20 different syntheticterpenoid-alkaloids for investigation as potential drugs. This work will be completed in collaboration withNanaimo Forest Products to determine preferred terpenes for modification and with the Centre for DrugResearch and Development in Vancouver for screening of new terpenoid-alkaloids for biological activity.