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Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo (2023)
Journal Article
Zhu, H., Zhu, W., Liu, Y., Gao, T., Zhu, J., Tan, Y., …Xu, S. (2023). Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo. European Journal of Medicinal Chemistry, 257, Article 115529. https://doi.org/10.1016/j.ejmech.2023.115529

A series of novel stilbene-based derivatives were designed and synthesized as tubulin/HDAC dual-target inhibitors. Among forty-three target compounds, compound II-19k not only exhibited considerable antiproliferative activity in the hematological cel... Read More about Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo.

Design, Synthesis, and Biological Evaluation of Novel Hybrids Containing Dihydrochalcone as Tyrosinase Inhibitors to Treat Skin Hyperpigmentation (2023)
Journal Article
Xue, S., Li, Z., Ze, X., Wu, X., He, C., Shuai, W., …Xu, S. (2023). Design, Synthesis, and Biological Evaluation of Novel Hybrids Containing Dihydrochalcone as Tyrosinase Inhibitors to Treat Skin Hyperpigmentation. Journal of Medicinal Chemistry, 66(7), 5099–5117. https://doi.org/10.1021/acs.jmedchem.3c00012

Excessive melanin deposition may lead to a series of skin disorders. The production of melanin is carried out by melanocytes, in which the enzyme tyrosinase performs a key role. In this work, we identified a series of novel tyrosinase inhibitor hybri... Read More about Design, Synthesis, and Biological Evaluation of Novel Hybrids Containing Dihydrochalcone as Tyrosinase Inhibitors to Treat Skin Hyperpigmentation.

Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation (2023)
Journal Article
Xie, S., Zhan, F., Zhu, J., Sun, Y., Zhu, H., Liu, J., …Xu, S. (2023). Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation. Angewandte Chemie International Edition, 62(13), Article e202217246. https://doi.org/10.1002/anie.202217246

Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in this study and was used to degrade the anaplastic lymphoma kinase (ALK) fusion prot... Read More about Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation.