| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1399068 | European Journal of Medicinal Chemistry | 2013 | 9 Pages |
•Analogue of DOTMP with 3 phosphonate groups and one amine group (DO3MP-EA) was studied as bone imaging agent.•Docking studies of known bone seekers were compared with DO3MP-EA to design it.•DO3MP-EA showed good bone seeking property for PET and SPECT applications.•It is potential therapeutic agent as amine can bind with specific drugs.
A cyclic tetraaza based bifunctional triphosphonate ligand 10-(2-aminoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-tris(methylenephosphonic acid) (DO3MP-EA) was synthesized as bone-seeking theranostic agent. The compound was characterized by spectroscopic techniques and labelled with 99mTc with more than 97% purity. Blood clearance of 99mTc labelled compound a quick wash out from the circulation. The compound was excreted mainly via kidneys and accumulation of 99mTc-DO3MP-EA in bone was 9.53 ± 1.06% of injected dose per gram of bone at 1 h. The preliminary CADD analysis confirms the efficacy of DO3MP-EA (G Score −7.005) as better binding agent for osteocalcin (pdb 1Q8H) rather than other known clinical agents. Subsequently stability constant of chelate with Ga(III) was found to be 18.6 which confirms its efficacy as 68Ga labelled PET radiopharmaceutical for bone.
Graphical abstractThree phosphonate groups and one amine group containing 1,4,7,10 tetraazadodecane derivative was synthesized and evaluated for bone seeking property. It showed promising results for SPECT and PET applications.Figure optionsDownload full-size imageDownload as PowerPoint slide
