133081-26-2Relevant articles and documents
PSMA inhibitor, application thereof and PSMA-targeting nuclide imaging reagent
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Paragraph 0045; 0049, (2020/06/20)
The invention belongs to the technical field of biological medicines, and particularly relates to a PSMA inhibitor, an application thereof and a PSMA-targeting nuclide imaging reagent. The PSMA inhibitor has a structure as shown in a formula I. The PSMA-targeting nuclide imaging reagent prepared by adopting EDDA as a co-ligand has good PSMA targeting property and affinity; high stability is realized in normal saline and mouse serum; meanwhile, the cell uptake amount is relatively high, and the metabolic performance is good. Therefore, the inhibitor has a good clinical application prospect in tumor imaging of targeted PSMA.
99mTc-labeled NGR-chlorambucil conjugate, 99mTc-HYNIC-CLB-c(NGR) for targeted chemotherapy and molecular imaging
Vats, Kusum,Satpati, Drishty,Sharma, Rohit,Kumar, Chandan,Sarma, Haladhar D.,Dash, Ashutosh
, p. 431 - 438 (2017/08/01)
Targeted delivery of chemotherapeutic drug at the tumor site enhances the efficacy with minimum systemic exposure. Towards this, drugs conjugated with peptides having affinity towards a particular molecular target are recognized as affective agents for targeted chemotherapy. Thus, in the present study, tumor-homing asparagine-glycine-arginine (NGR) peptide ligand was conjugated to DNA alkylating nitrogen mustard, chlorambucil (CLB). The peptide-drug conjugate (PDC), CLB-c(NGR), was radiolabeled with 99mTc-HYNIC core to trace its pharmacokinetics and biodistribution pattern. In vitro cell-binding studies of 99mTc-HYNIC-CLB-c(NGR) were conducted in murine melanoma B16F10 cells. The cytotoxicity studies conducted by incubation of the peptide/drug/PDC with B16F10 cells demonstrated enhanced cytotoxic effect of PDC in comparison to either the peptide or the drug alone. In vivo biodistribution studies in C57BL6 mice bearing melanoma tumor showed maximum tumor uptake at 30?minutes pi (2.45?±?0.28% ID/g), which reduced to 0.77?±?0.1% ID /g at 3?hours pi. The radiotracer being hydrophilic cleared rapidly from the heart, lungs, liver, and muscle. The tumor-to-blood and tumor-to-muscle ratios improved with time. This study opens avenues for conjugation of other targeting peptides with the drug CLB for enhanced toxicity at the diseased site.
Syntheses and biological evaluation of 99mTc-HYNIC-fatty acid complexes for myocardial imaging
Mathur, Anupam,Sharma, Abhishek K.,Murhekar,Mallia, Madhava B.,Pawade, Shital,Sarma,Chaudhari, Pradip,Sachdev,Banerjee, Sharmila
, p. 93374 - 93385 (2015/11/17)
The aim of the present study is to identify a 99mTc-labeled fatty acid tracer which could be a possible substitute of the widely used 123I-labeled fatty acids in studying myocardial metabolism and in detection of myocardial abnormalities in high-risk patients. The relevance of the study stems from the fact that in terms of wider applicability, a 99mTc-tracer is expected to be more advantageous compared to that of a 123I-based one. Two fatty acid (FA)-hydrazinopyridine-3-carboxylic acid (HYNIC) conjugates (11C-FA-HYNIC and 12C-FA-HYNIC) were synthesized and radiolabeled with 99mTc using two different co-ligands system viz. tricine/ethylenediamine diacetic acid (EDDA), and tricine/trisodium triphenylphosphine-3,3′,3′′-trisulfonate (TPPTS), to yield four radiolabeled complexes. While all four 99mTc-HYNIC-complexes showed uptake in the myocardium, 12C-FA-HYNIC-99mTc-EDDA complex showed higher uptake and retention in myocardium compared to other complexes. In general, uptake of the 99mTc-complexes in non-target organs was lower than that of 125I-iodophenyl pentadecanoic acid (IPPA). The 12C-FA-HYNIC-99mTc-EDDA complex, additionally exhibited lower liver accumulation compared to that of 125I-IPPA. Though these features were favorable for cardiac imaging, the heart-to-blood ratio of the complexes were low (99mTc-EDDA complex in Swiss mouse showed delineation of its myocardium from proximal non-target organs. The results merit further screening of synthetically modified 99mTc-HYNIC fatty acids for myocardial imaging.
Synthesis and stability evaluation of new HYNIC derivatives as ligands for Technetium-99m
Joyard, Yoann,Bischoff, Laurent,Levacher, Vincent,Papamicael, Cyril,Vera, Pierre,Bohn, Pierre
, p. 208 - 214 (2014/05/20)
An efficient synthetic route to prepare two new HYNIC derivatives with a 2-nitroimidazole moiety designed for tumor hypoxia imaging is described. During the course of the synthesis, the optimization of N-alkylation reaction of 2- nitroimidazole with propargyl bromide is reported to favor the formation of the terminal alkyne versus allene. Thereafter, the two ligands were used with tricine/EDDA to complex 99mTc. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.
Synthesis of radiolabeled cytarabine conjugates
Lagisetty, Pallavi,Vilekar, Prachi,Awasthi, Vibhudutta
supporting information; experimental part, p. 4764 - 4767 (2010/04/26)
N4-Modified, novel Ara-C conjugate capable of radiolabeling with gamma ray-emitting (99mTc) as well as positron emitting (18F) radionuclides, that is, N4-hydrazine derivative was synthesized. The radiolabeling of N4-(hydrazinonicotin
Technetium-99m-labeling and synthesis of thymidine analogs: Potential candidates for tumor imaging
Teng, Bao,Bai, Yunpeng,Chang, Yu,Chen, Shizhen,Li, Zhaolong
, p. 3440 - 3444 (2008/02/10)
The technetium-99m-labeling and synthesis of a series of thymidine analogs were studied. The target molecules were obtained by using 6-hydrazinopyridine-3-carboxylic acid (HYNIC) as a bifunctional coupling agent and using N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) and ethylenediamine-N,N′-diacetic acid (EDDA) as coligands. The effects of different spacers between thymidine analog with HYNIC on radiochemical yield were also studied.
