3-O-Phosphate ester conjugates of 17-β-O-{1-[2-carboxy-(2-hydroxy-4-methoxy-3-carboxamido)anilido]ethyl}1,3,5(10)-estratriene as novel bone-targeting agents
作者:Shama Nasim、Ashish P. Vartak、William M. Pierce、K. Grant Taylor、Ned Smith、Peter A. Crooks
DOI:10.1016/j.bmcl.2010.10.023
日期:2010.12
A series of 3-O-phosphorylated analogs (4–10) of a novel bone-targeting estradiol analog (3) were synthesized after a thorough study of the reaction of 3 with a selection of phosphoryl chlorides under a variety of reaction conditions. Evaluation of these novel phosphate analogs for affinity for hydroxyapatite revealed that they bind with equal or higher affinity when compared to the bone tissue accumulator
一系列3- ø磷酸化的类似物(4 - 10)的新型靶向骨的雌二醇类似物(的3)中的反应的深入研究后合成3用在各种反应条件的选择磷酰基氯化物。这些新型磷酸盐类似物对羟基磷灰石亲和力的评估表明,与骨组织蓄积剂四环素相比,它们以相等或更高的亲和力结合。