Acyclonucleoside iron chelators of 1-(2-hydroxyethoxy)methyl-2-alkyl-3-hydroxy-4-pyridinones: Potential oral iron chelation therapeutics

被引:7
作者
Liu, G [1 ]
Men, P [1 ]
Kenner, GH [1 ]
Miller, SC [1 ]
Bruenger, FW [1 ]
机构
[1] Univ Utah, Div Radiobiol, Salt Lake City, UT 84108 USA
关键词
acyclonucleoside; pyridinones; iron chelators; desferrioxamine; therapeutics;
D O I
10.1081/NCN-120030718
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The method of synthesizing acyclonucleoside iron chelators is both convenient and cost effective compared to that of synthesizing ribonucleoside iron chelators. The X-ray crystal structural analysis shows that the 2-hydroxyethoxymethyl group does not affect the geometry of the iron chelating sites. Therefore, the iron binding and removal properties of the acyclonucleoside iron chelators should remain similar to the ribonucleoside iron chelators, which is confirmed by the titration and competition reaction of the acyclonucleoside chelators with iron and ferritin, respectively. The acyclonucleoside iron chelators are more lipophilic with measured n-octanol and Tris buffer distribution coefficients than ribonucleoside iron chelators.
引用
收藏
页码:599 / 611
页数:13
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