- 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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- Concise total synthesis of aplysinellamides A and B
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Concise and efficient total syntheses of bromotyrosine-derived metabolites aplysinellamides A and B, isolated from Australian marine sponge Aplysinella sp., have been accomplished in seven steps. A condensation between cinnamic acid and Boc-D-lysine methyl ester was applied to form the amide skeleton as a key step.
- Gan, Haifeng,Huang, Yu,Feng, Weiyang,Zhu, Wentong,Guo, Kai
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p. 336 - 339
(2015/08/11)
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- Synthesis of Unnatural Amino Acids
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This communication presents efficient synthetic procedures for the D and L isomers of Nα-tert-butyloxycarbonyl-Nε-benzyloxycarbonyl-Nε-isopropyllysine dicyclohexylamine salt (Nα-Boc-Nε-Z-Ilys DCHA salt), the D and L isomers of Nα-tert-butyloxycarbonyl-Nεnicotinoyllysine (Nα-Boc-Niclys), β-(3-quinolyl)-D,L-alanine (3-Quinal), and the resolution into the D and L isomers of 3-Quinal.
- Acosta, C. Kirk,Bahr, Martin L.,Burdett, James E.,Cessac, James W.,Martinez, Rudy A.,et al.
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p. 914 - 934
(2007/10/02)
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