- Novel aminopeptidase N inhibitors with improved antitumor activities
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A series of aminopeptidase N (APN) inhibitors were designed and synthesized. Enzyme inhibitory, docking and antiproliferative studies were performed to evaluate the derived molecules. Molecule D15, with IC50 values of 10.9 μM, showed the best performance in the APN enzymatic inhibition assay. The binding pattern of molecule D9 and D15 in the active site of APN was predicted by docking studies. Hydrophobic and H-bond interactions were discovered to make key roles in the ligand-receptor bindings. Compared with the previous C7, several molecules such as D9, D14 and D15, exhibited significantly improved activities in inhibiting the growth of HL-60, ES-2, A549 and PLC cell lines.
- Wang, Qiang,Shi, Qiao,Huang, Lu
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- Decomposition of copper-amino acid complexes by oxalic acid dihydrate
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A facile approach to the synthesis of some side-chain-protected amino acids via oxalic acid dihydrate as the copper sequestering reagent is presented. The copper in the amino acid complex reacted with oxalic acid dihydrate to form insoluble cupric oxalate, with the free amino acid released. Compared with conventional methods, this method is convenient, inexpensive, and environmentally friendly.
- Liu, Yi,Jia, Genguang,Ling, Xin,Lan, Nuo,Zheng, Youguang,Li, Sai,Zhang, Ling,Liu, Ling,Zhang, Rongli,Xue, Yunsheng
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p. 557 - 559
(2012/08/08)
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