کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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17881 | 42703 | 2008 | 7 صفحه PDF | دانلود رایگان |
We achieved an effective way of controllable regioselective acylation of primary or secondary hydroxyl group of floxuridine with different enzymes. Polymerizable 5′-O-acyl-floxuridine derivatives were synthesized by CAL-B (immobilized lipase from Candida antarctica) in acetonitrile or subtilisin in pyridine, and the 3′-O-acyl-floxuridine derivatives by PSL-C (Pseudomonas cepacia, immobilized) in THF with high selectivity and yields. These resulting monomers were subjected to the further transformations in the second step, i.e. chemo-polymerization in DMF initiated by azobisisobutyronitrile to give polymeric prodrugs with the same backbone and different branch position, and enzymatic conjugation of d-galactose for the synthesis of d-galactose–floxuridine conjugates with acylation position-diversity, which were potential targeting drugs.
Journal: Enzyme and Microbial Technology - Volume 42, Issue 5, 4 April 2008, Pages 414–420