183383-58-6Relevant articles and documents
PET bone imaging agent precursor and synthesis method thereof
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Paragraph 0059, (2019/12/10)
The invention discloses a PET bone imaging agent precursor, wherein a linking agent tripolyethanol is introduced between a macrocyclic polyamine ligand and a targeting carrier diphosphonic acid, and the diphosphonic acid bone-seeking group with targeting effect can form the macrocyclic polyamine cooperation group of a stable chelate with a plurality of metal nuclides so as to form a bone imaging agent. According to the present invention, the synthesized precursor compound contains the bone-seeking group (diphosphonic acid) and the cooperation group (DOTA), and the two functional groups are linked by PFG3, such that the precursor compound has remarkable structural characteristics; the precursor compound has strong bone-seeking property, and can form a complex (marker) with kinetic and thermodynamic stability with metal nuclides; the marker formed by marking the precursor with different metal nuclides can be used as a bone imaging agent (marked with Cu, Ga and other positron emission metal nuclides) with powerful functions, and can further be used as an ideal bone tumor treatment drug (marked with In, Y, Zr, Sm and other radioactive treatment metal nuclides).
An osteoclast-targeting agent for imaging and therapy of bone metastasis
Liu, Wei,Hajibeigi, Asghar,Lin, Mai,Rostollan, Cynthia L.,Kovacs, Zoltan,Oez, Orhan K.,Sun, Xiankai
experimental part, p. 4789 - 4793 (2009/05/26)
A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N′,N″,N?-tetraac etic acid, DOTA) and an osteoclast-targeting moiety (bisphosphonate) was designed and synthesized. The 111In-labeled complex of DO3A-BP showed significantly elevated uptake in osteoclasts compared to the undifferentiated adherent bone marrow derived cells. Biodistribution studies revealed a favorable tissue distribution profile in normal mice with high bone uptake and long retention, and low or negligible accumulation in non-target organs.
Novel synthesis of bis(phosphonic acid)-steroid conjugates
Page,McKenzie,Gallagher
, p. 3704 - 3708 (2007/10/03)
An efficient synthesis has been realized for several members of a new class of potential bone resorption inhibitors consisting of steroidal oestrogenic units linked at the 3 and 17 positions to a geminal bisphosphonate moiety through an ester linkage of variable length. The convergent synthesis utilizes benzyl bisphosphonates, transesterification, and Meldrum's acid chemistry and has the potential to allow many oestrogenic derivatives as well as other biologically active compounds to be coupled to the geminal bisphosphonate moeity.