Development of a concise synthesis of analogs derived from Amaryllidaceae alkaloids family******************

本提案的重点是UQAM和IntelliSyn制药公司之间的密切合作，以评估和生产在一个旨在全合成高生物活性小天然产物的基础项目中获得的类似物。本研究的主要目的是开发一种简洁、高效的合成途径，以制备一类重要的生物活性生物碱——amaryllidiaceae科的类似物。该家族的天然产物，如石蒜碱、水仙素、pancrastistatin及其天然衍生物，因其对几种癌症具有重要的生物活性而闻名。这些化合物的优点是它们是小的生物活性分子，可以通过全合成大规模地获得，这是紫杉醇或长春花碱等复杂药物所无法做到的。开发了一种新的生物碱提取方法；这种方法可以在几个步骤中生产出含有关键生物活性成分的主要核心。这种新的合成方法产生了尚未由已知合成途径产生的类似物，并可能开辟新的机会。与IntelliSyn制药等知名公司合作，将有助于我们生产出具有所需物理化学特性的有趣支架

This present proposal focuses on a close collaboration between UQAM and IntelliSyn pharma to valorize and produce analogs that have been obtained during a fundamental project aiming the total synthesis of highly bioactive small natural products. The main objective is to develop a concise and efficient synthetic pathway to produce analogs derived from Amaryllidaceae family, an important class of bioactive alkaloids. Natural products from this family such as lycoricidine, narciclasine, pancrastistatin and their natural derivatives are known for their important bioactivity against several cancers. These compounds have the advantage to be small bioactive molecules that can be obtained in large scale by total synthesis, which is not the case with complex drugs such as taxol or vinblastine. A new approach of these alkaloids has been developed; this method allows producing in few steps their main cores containing the crucial bioactive moieties. This new synthetic approach generates analogs that were not yet produced by known synthetic pathways and could open-up novel opportunities. Collaboration with a recognized company such as IntelliSyn pharma will help us to produce interesting scaffolds with required physico-chemical properties.**