Design,synthesis and evaluation of novel metalloproteinase inhibitors based on l-tyrosine scaffold |
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Authors: | Xian-Chao Cheng Run-Ling Wang Zhen-Ke Dong Jing Li Yao-Yuan Li Rong-Rong Li |
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Institution: | Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China |
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Abstract: | A series of novel l-tyrosine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 (MMP-2) and histone deacetylase 8 (HDAC-8). The results showed that these l-tyrosine derivatives exhibited inhibitory profiles against MMP-2 and HDAC-8. The compounds 6h (IC50 = 0.013 ± 0.001 μM) and 6j (IC50 = 0.017 ± 0.001 μM) were equal potent MMP-2 inhibitors to the positive control NNGH (IC50 = 0.014 ± 0.001 μM). As for HDAC-8 inhibition, some of the hydroxamate compounds, such as 6d (IC50 = 3.6 ± 0.2 μM) and 6c (IC50 = 5.8 ± 0.5 μM), were equal potent to the positive control SAHA (IC50 = 1.6 ± 0.1 μM). Structure–activity relationships were also briefly discussed. |
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