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ID: ALA1287764

Journal: Bioorg Med Chem Lett

Title: 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.

Authors: Nasim S, Vartak AP, Pierce WM, Taylor KG, Smith N, Crooks PA.

Abstract: 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, tetracycline.

CiteXplore: 21055931

DOI: 10.1016/j.bmcl.2010.10.023