Pd-catalyzed Suzuki-Miyaura coupling reactions in the synthesis of 5-aryl-1-[2-(phosphonomethoxy)ethyl]uracils as potential multisubstrate inhibitors of thymidine phosphorylase |
| |
Authors: | Karel Pomeisl,Antoní n Holý ,Radek Pohl |
| |
Affiliation: | Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 166 10 Prague, Czech Republic |
| |
Abstract: | -5-Aryl-1-[2-(phosphonomethoxy)ethyl]uracils were prepared via Pd-catalyzed Suzuki-Miyaura coupling reaction of the appropriate 5-bromouracil derivative with a series of arylboronic acids followed by deprotection. These compounds were designed as potential multisubstrate inhibitors of thymidine phosphorylase based on an assumption that the potential hydrophobic effect of the aryl groups might modify the inhibitory effect towards this enzyme and they may also demonstrate cytostatic activity. |
| |
Keywords: | Acyclic nucleoside phosphonates Thymidine phosphorylase Suzuki coupling Pyrimidine |
本文献已被 ScienceDirect 等数据库收录! |