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.
Original language | English (US) |
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Pages (from-to) | 7450-7453 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 24 |
DOIs | |
State | Published - Dec 15 2010 |
Bibliographical note
Funding Information:Financial support from Pradama, Inc., and the Kentucky Science and Technology Corporation is gratefully acknowledged. W.M.P., K.G.T. and P.A.C. have a financial interest in Pradama, Inc.
Keywords
- Bone-targeting agents
- Hydroxyapatite binding
- Osteoporosis
- Phosphate esters