[76Br]Bromodeoxyuridine PET in tumor-bearing animals

Gardelle, O; Roelcke, Ulrich; Vontobel, Peter; Crompton, N. E. A.; Guenther, Ilonka; Bläuenstein, Peter; Schubiger, August P.; Blattmann, H.; Ryser, Jean E.; Leenders, Klaus L.; Kaser‐Hotz, Barbara

doi:10.1016/s0969-8051(00)00189-x

Cited by 23 publications

(15 citation statements)

References 20 publications

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“…The solvent was removed under reduced pressure and the pale-yellow residue co-evaporated once with MeOH (30 mL). The crude mixture was purified by silica gel chromatography using a gradient of CH 2 (18). Compound 18 was prepared by a procedure similar to that described for compound 11, except that compound 7 was used instead of compound 5.…”

Section: -(2-aminoethyl)-1-((2r4r5r)-tetrahydro-4-hydroxy-5-(hydromentioning

confidence: 99%

“…A representative synthesis is described in detail for the complex formation reaction of ligand 15. All metal complexes were further purified by semipreparative HPLC on a reversed-phase C 18 column and obtained in excellent yields as light powders.…”

Section: Rhenium Complex Synthesesmentioning

confidence: 99%

“…[17,18] This latter application has led to considerable interest in the [M(CO) 3 ] + 1 core with M = 99m Tc or Re. [19][20][21][22][23] The corresponding technetium and rhenium precursors [M(CO) 3 (H 2 O) 3 ] + 1 can be conveniently accessed by synthetic procedures, are water soluble, and the three aqua ligands are labile and can readily undergo ligand exchange.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes

Bartholomä¹,

Vortherms²,

Hillier³

et al. 2010

ChemMedChem

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Nucleoside analogues are extensively used in the treatment of cancer and viral diseases. The antiproliferative properties of organorhenium(I) complexes, however, have been scarcely explored to date. Herein we present the syntheses, characterization, and in vitro evaluation of Re(I)(CO)(3) core complexes of thymidine and uridine. For the binding of the Re(I)(CO)(3) core, a tridentate dipicolylamine metal chelate was introduced at positions C5', C2', N3, and C5 with spacers of various lengths. The corresponding organometallic thymidine complexes were fully characterized by IR and NMR spectroscopy and mass spectrometry. Their cytotoxicity was assessed against the A549 lung carcinoma cell line. Toxicity is dependent on the site and mode of conjugation as well as on the nature and the length of the tether. Moderate toxicity was observed for conjugates carrying the rhenium moiety at position C5' or N3 (IC(50)=124-160 microM). No toxicity was observed for complexes modified at C2' or C5. Complex 53, with a dodecylene spacer at C5', exhibits remarkable toxicity and is more potent than cisplatin, with an IC(50) value of 6.0 microM. To the best of our knowledge, this is the first report of the antiproliferative properties of [M(CO)(3)](+1)-nucleoside conjugates. In competitive inhibition experiments with A549 cell lysates and purified recombinant human thymidine kinase 1 (hTK-1), enzyme inhibition was observed for complexes modified at either N3 or C5', but our results suggest that the toxicity cannot be attributed solely to interaction with hTK-1.

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Section: -(2-aminoethyl)-1-((2r4r5r)-tetrahydro-4-hydroxy-5-(hydromentioning

confidence: 99%

Section: Rhenium Complex Synthesesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes

Bartholomä¹,

Vortherms²,

Hillier³

et al. 2010

ChemMedChem

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“…The first radiotracer of cellular proliferation studied and visualised in vivo was [ 11 C]thymidine, synthesised by Christman and Brookhaven [39], and it was proposed to visualise cellular proliferation by other authors [49,52] but it is used less every day because of its fast catabolism and metabolic instability [6,52]. Several halo- [56]. Wagner et al [49] have shown that in vivo incorporation of [ 18 F]fluorodeoxyuridine (FudR) is correlated with cellular proliferation in an animal model for pancreatic cancer.…”

Section: Cellular Proliferationmentioning

confidence: 99%

Use of radionuclides in cancer research and treatment

Macias

2009

Clin Transl Oncol

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Cancer occurs as a result of misregulation of cell growth, which appears to be a consequence of alteration in the function of oncogenes and tumour suppressor genes. Ionising radiation has been used, since the discovery of X-rays in 1896 by Roentgen, both in cancer research and treatment of the disease. The main purpose of cancer research is to understand the molecular alterations involved in the development and progression of the disease in order to improve diagnosis and develop personalised therapies, by focusing on the features of the tumoral cell and the biological events associated to carcinogenesis. Radioisotopic techniques have been used routinely for in vitro research in the molecular and cellular biology of cancer for more than 20 years and are in the process of being substituted by alternative non-radioactive techniques. However in vivo techniques such as irradiation of cells in culture and/or experimental animal models and radioactive labelling are in development, due in part to advances in molecular imaging technologies. The objective of this review is to analyse in an integrative way the applications of ionising radiation in cancer research and therapy. It had been divided into two parts. The first one will approach the techniques applied to cancer research and the second will summarise how ionising radiation is applied to the treatment of neoplastic disease.

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“…Radiolabelled iododeoxyuridine (IdUrd) and other thymidine (dThd) analogues, labelled with gamma or positron emitters such as 11 C, 124 I, or 76 Br, have been explored for non-invasive scintigraphy of tumour cell division in patients [1,2,3,4]). Furthermore, use of radioIdUrd has been considered for cancer therapy based on its potential to specifically target cytotoxic Auger radiation into DNA of dividing cells [5].…”

Section: Introductionmentioning

confidence: 99%

Preclinical Auger and gamma radiation dosimetry for fluorodeoxyuridine-enhanced tumour proliferation scintigraphy with [123I]iododeoxyuridine

Buchegger

Vieira

Blaêuenstein

et al. 2003

Eur J Nucl Med Mol Imaging

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Animal experiments have shown that short blocking of thymidine (dThd) synthesis with fluorodeoxyuridine (FdUrd) results in significantly increased DNA incorporation of [(125)I]iododeoxyuridine ([(125)I]IdUrd) in tumour and rapidly cycling tissues. Based on these results, we give an Auger and gamma radiation dosimetry estimate for a scintigraphy study in glioblastoma patients using [(123)I]IdUrd. The Auger radiation dosimetry calculated for patients is based on measurement of DNA-incorporated [(125)I]IdUrd in rapidly dividing tissues in nude mice xenografted with human glioblastoma. Further data obtained 0.5, 6 and 24 h after injection of [(125)I]IdUrd allowed calculation of the additional gamma radiation exposure using MIRDOSE3.1. High gradients of radioactivity concentration between dividing and non-dividing tissues were observed 6 and 24 h after injection of [(125)I]IdUrd combined with FdUrd pretreatment. While the estimated Auger radiation absorbed doses of [(123)I]IdUrd in six rapidly cycling normal tissues in patients are low, the equivalent doses become significant with application of the recommended preliminary radiation weighting factor (W(R)) of 20 for stochastic effects of DNA-associated Auger radiation. Using the latter W(R), extrapolation of the animal results to the proposed patient injection with 300 MBq [(123)I]IdUrd combined with FdUrd pretreatment indicates that the effective dose will be 5.42 mSv, including 1.67 mSv from Auger and 3.75 mSv from gamma radiation. The predicted Auger radiation effective dose for patients undergoing [(123)I]IdUrd scintigraphy will be significant if the enhancement of DNA incorporation that is achieved by means of FdUrd pretreatment is similar to that obtained in animals.

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[76Br]Bromodeoxyuridine PET in tumor-bearing animals

Cited by 23 publications

References 20 publications

Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes

Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes

Use of radionuclides in cancer research and treatment

Preclinical Auger and gamma radiation dosimetry for fluorodeoxyuridine-enhanced tumour proliferation scintigraphy with [123I]iododeoxyuridine

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[76Br]Bromodeoxyuridine PET in tumor-bearing animals

Cited by 23 publications

References 20 publications

Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)3 Thymidine Complexes

Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)3 Thymidine Complexes

Use of radionuclides in cancer research and treatment

Preclinical Auger and gamma radiation dosimetry for fluorodeoxyuridine-enhanced tumour proliferation scintigraphy with [123I]iododeoxyuridine

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Product

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Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes

Synthesis, Cytotoxicity, and Insight into the Mode of Action of Re(CO)₃ Thymidine Complexes