Our laboratory focuses on three major research areas: development of novel methodologies, addressing the unmet needs for efficient medicine synthesis and application of powerful chemical tools to answer important biology questions.
Though considered as a mature science, the synthesis of natural product and pharmacophore remains unsatisfactory in terms of the overall atom-, step- and cost-economy. Furthermore, as the pharmaceutical industry has put more and more emphasis on bio-conjugates, in particular, antibody-drug conjugates (ADC), the high demand for reliable conjugation methods has become an urgent issue that needs to be addressed. As one of the fundamental research activities in our lab, the novel methodology discovery program enables efficient laboratorial and industrial scale synthesis of chemical entities with biological activity.
In addition to methodology development and targeted synthesis, we are also engaged in chemical biology research. We have a great interest in antimicrobial and antiplasmodial research. We have targeted several natural products and their analogues for total chemical synthesis and have been trying to explore their medicinal applications. In collaboration with microbiologists and infectious disease experts, we leverage our synthetic strength and medicinal chemistry knowledge to design specific antibiotics and manipulate their activity at molecular levels.
Craig, W.; Chen, J. Richardson, D.; Thorpe, R., Yuan, Y.* A Highly Stereoselective and Scalable Synthesis of L-allo-Enduracididine. Org. Lett., 2015, 17, 4620-4623. Link
Zheng, Y.; Cleaveland, J.; Richardson, D.; Yuan, Y.* An Organocatalysis Based Carbocyclic Spiroindoline Synthesis Enables Facile Structure−Activity Relationship (SAR) Study at C2 Position. Org. Lett., 2015, 17, 4240-4243. Link
Zheng, Y.; Liu, M., Yuan, Y.* A Very Mild and Selective Method for O-Benzoylation of Hydroxamic Acids. Tetrahedron Lett., 2014, 55, 4404-4406. Link