Li Cheng-cheng's task force successfully developed an asymmetric all-synthetic route of autumn daffodil base.

Colchicine is the first internationally reported natural product that blocks microtoprotein conversion, which in turn causes cell death.
daffodils have many excellent biological activities, such as special-effect prescription drugs for acute gout and the only FDA-approved drug for familic Mediterranean fever that patients need to take for life.
, however, due to the high toxicity of autumn daffodils to normal human tissue, severe cases can lead to kidney failure and death.
Akio daffodils are also landmark star molecules in the history of full synthesis, and their full synthesis is quite difficult: how to three-dimensional selectivity, regional selectivity, and high-reflection selectivity to build a 6-7-7 three-ring system, with great synthesis challenges.
Since its separation, it has attracted the research interest of many synthetic chemists in the world, so far, there are four full synthesis and more than a dozen forms of full synthesis reports, but the synthesis route is cumbersome and inefficient, it is difficult to meet various research needs.
among them, Professor Woodward of Harvard University (Nobel Laureate), 23 steps, unknown yield, and Professor Eschenmoser of the Scripps Institute (world-renowned chemist), 22 steps, with a total yield of 0.00006%.
Therefore, the development of an efficient and concise autumn daffodil synthesis program, and through structural modification synthesis of its similar substances, looking for high-efficiency low-toxic, with independent intellectual property rights of drug-led compounds, will have very important academic and social significance, but also contains huge business opportunities.
Recently, Li Chengcheng's team developed a new strategy of efficient and concise synthesis, starting with cheap, commercially available raw materials, using the in-molecular ring plus reaction previously reported in this topic to quickly build a 6-7 with greater synthesis challenges. -7 three-ring core skeleton, only 9 steps, you can complete the asymmetric full synthesis of autumn daffodil base (g-level preparation, the selectivity of the reflection is greater than 99%), the total yield of up to 9%, which is also the natural product synthesis history in the international shortest and most efficient synthesis route.
team also completed the first asymmetric full synthesis of Demecolcinone and Metacolchicine, natural products of the Akio daffodil family, and determined their absolute construction.
In addition, the team has completed dozens of rapid synthesis of autumn daffodils and similars, and anti-tumor activity tests, the results show that the compound 30 pairs of human lung cancer cells, breast cancer cells, colon cancer cells, etc. have a significant inhibitory effect, reaching the level of 3 namole (nM), than the acacie base itself is excellent.
Further data on the effects of microcytoproteins in breast cancer cells, cell skeleton morphology change experiments, in-body enzyme dynamics experiments, etc., show that the direct knotting effect of compound 30 and microphedrine and in-body inhibition of microtone polymerization are stronger than that of acacian.
the work was recently published in the world's leading chemical science journal (Chem.Sci.2017, Advance Article).
research has laid the foundation for further pharmaceutical research on anti-tumor innovative drugs with independent intellectual property rights.
Dr. Chen Bo, a postdoctoral student in the Research Group of Li Cheng,and Dr. Liu Xin, a Ph.D. student at the University of Macau, also made important contributions to the paper, including the co-author of the paper, graduate student Hu Yajian, undergraduate Lu Wei, and postdoctoral student Yu Long, dr. Li Cheng-chun is the sole communication author, and the Southern University of Science and Technology is the first author and communication author unit.
bioactivity was carried out in collaboration with Professor Ye Wencai of Jinan University.
the study was supported by the National Fund Committee's Outstanding Youth Fund, the National "Million People's Program", the Guangdong Province's 100 million project leaders' program, and the Shenzhen Science and Technology Commission.
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