Publications by authors named "Geshuyi Chen"

Since the initial report in 1975, the Shono oxidation has become a powerful tool to functionalize the α position of amines, including proline derivatives, by electrochemical oxidation. However, the application of electrochemical Shono oxidations is restricted to the preparation of simple building blocks and homogeneous Shono-type oxidation of proline derivatives remains challenging. The late-stage functionalization at proline residues embedded within peptides is highly important as substitutions about the proline ring are known to affect biological and pharmacological activities.

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Article Synopsis
  • Structure modification of drugs, particularly late-stage functionalization (LSF), is effective for optimizing lead compounds, and this study focused on Cu-catalyzed C-H LSF of 5-nitrofuran drugs.
  • Multiple modifications were performed on the 5-nitrofuran drugs, including hydroxylation, methylation, azidination, cyanation, and arylation, and the antibacterial activities of the new compounds were tested.
  • Among the modified compounds, compounds 1 and 18 showed the highest antibacterial activity, while cell cytotoxicity assays were conducted on potent compounds and the parent drug to assess safety.
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Introduction: Bone marrow mesenchymal stem cells (BMSCs) are a promising cell type for tissue engineering, however, the application of BMSCs is largely hampered by the limited number harvested from bone marrow cells. The methods or strategies that focused on promoting the capacity of BMSCs expansion become more and more important. Tanshinone IIA (Tan IIA), the main active components of Danshen, has been found to promote BMSCs proliferation, but the underlying mechanism is still unclear.

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Nitrogen heterocycle represents a ubiquitous skeleton in natural products and drugs. Late-stage C(sp)-H bond functionalization of N-heterocycles with broad substrate scope remains a challenge and of particular significance to modern chemical synthesis and pharmaceutical chemistry. Here, we demonstrate copper-catalysed late-stage C(sp)-H functionalizaion of N-heterocycles using commercially available catalysts under mild reaction conditions.

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