Abstract

Cyclam based hybrid compound for imaging and therapy of Bone Metastasis

Author(s): Tyagi Amit Kumar1*, Sharma Rajbala1, Sharma Himanshu2, Katara Antariksh3

Present study shows the synthesis of 7 however, an alternative route was used in this work, in which a commercially available intermediate, 5 (1,4,7,10-tetraazacyclododecane-1,4,7- tris(tbutyl) acetate: DO3A-t-Bu-ester) was used as starting material instead of cyclam and a higher overall yield (77%) was achieved. A convergent approach was chosen to synthesize the hybrid ligand, in which the derivatives of a bisphosphonate and Cyclam metal chelator (7) were synthesized. The carboxylate acid substituted bisphosphonate, 3-bis-(dibenzyloxyphosphoryl) propanoic acid (3), was synthesized by a literature procedure with an overall yield of 27%. Blood kinetics findings in rabbits are an indication of the excellent in vivo stability of the 99mTc- AI and non-osseous tissue uptake of 99mTc-AI is minimal and when assessed with its rapid blood clearance accounts for the low soft tissue activity. Rapid incorporation of phosphonates into calcified tissue leads to their short presence in the circulation. By Receptor binding studies of Scatchard plot analysis revealed affinity of the AI on tumor cell lines (Soas-2) and Scintigraphy observed that the uptake of the conjugate was faster than that of the ALN and MDP alone. ______________________________________________________________________________

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