Preparation and Biological Evaluation of &lt;sup&gt;99m&lt;/sup&gt;Tc-Labelled Phenazine Dioxides as Potential Tracers for Hypoxia Imaging

Fernández, Soledad; Berchesi, Agustina; Tejería, Emilia; Sanz, I.; Cerecetto, Hugo; González, Mercedes; Lavaggi, María Laura; Rey, Ana

doi:10.2174/1874471007666141202145948

Cited by 3 publications

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“…For this purpose, different chemical entities have been used, i.e., CuSO 4 , surface-active chemicals, ionophores, triazine, lipids, saponins, and tannins. For almost 20 years, our research group has been working on the development and biological evaluation of different N -oxide-containing aromatic heterocycles [13,14,15,16,17,18]. Among the most relevant biological activities, we have found anti-protozoa activity in phenazine dioxide [19], quinoxaline dioxide [20], indazole N -oxide [21], benzofuroxan [22,23], benzimidazole dioxide [24], and furoxan derivatives [23,25].…”

Section: Introductionmentioning

confidence: 99%

Identification of N-Oxide-Containing Aromatic Heterocycles as Pharmacophores for Rumen Fermentation Modifiers

et al. 2019

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Different strategies have been used to mitigate greenhouse gas emissions from domesticated ruminants, including the removal of protozoa (defaunation). The objective of the present work was to analyze the potential of different N-oxide-containing aromatic heterocycles with known antiprotozoal activity as rumen-gas-abating agents. Nineteen pure compounds, belonging to seven different N-oxide chemotypes from our chemo-library were studied together with monensin in an in vitro rumen simulation assay. Fermentation profiles, i.e., gas production, pH, and short carboxylic acid concentrations, were compared to an untreated control at 96 h post inoculation. In our study, we investigated whole-ruminal fluid, with and without compound treatments, by NMR spectroscopy focusing on concentrations of the metabolites acetate, propionate, butyrate, and lactate. From data analysis, three of the compounds from different N-oxide chemotypes, including quinoxaline dioxide, benzofuroxan, and methylfuroxan, were able to diminish the production of gases such as monensin with similar gas production lag times for each of them. Additionally, unlike monensin, one methylfuroxan did not decrease the rumen pH during the analyzed incubation time, shifting rumen fermentation to increase the molar concentrations of propionate and butyrate. These facts suggest interesting alternatives as feed supplements to control gas emissions from dairy ruminants.

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Section: Introductionmentioning

confidence: 99%

Identification of N-Oxide-Containing Aromatic Heterocycles as Pharmacophores for Rumen Fermentation Modifiers

et al. 2019

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“…For specifically detecting solid tumors, technetium-99m combined with phenazine N,N'-dioxides are an efficient way because these molecules have the capacity to be bioreduced under hypoxic conditions (Rey et al, 2015).…”

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“…One of them was 99m Tctricarbonyl-(2-amino-5,10-dioxide-7(8)-fluorophenazine), Tc-FZ, that displayed adequate tumor/non-tumor ratios in a model of lung carcinoma (Rey et al, 2015).…”

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<strong>99m Tc-Tricarbonyl- (2-amino- 5,10-dioxide- 7(8)-fluorophenazine) as Probe for Mammary Hypoxic-tumors Imaging</strong>

Afonso

Cabral

González

et al. 2017

Proceedings of 3rd International Electronic Conference on Medicinal Chemistry

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Abstract:Our group has previously reported potential new radiopharmaceuticals, i.e. 99m Tctricarbonyl-(2-amino-5,10-dioxide-7(8)-fluorophenazine), Tc-FZ, with the ability to detect hypoxic tumoral tissues. Previously, this probe was used to detect solid tumors, employing a model of lung carcinoma generated by inoculation of 3LL Lewis murine cells in C57BL/6 mice. The results revealed an adequate tumor/muscle ratio, 3.8 at 2 h post-injection (p.i.), with lower tumor/blood ratio, i.e. 0.6 at 2 h p.i.. Due to some models of breast cancer also being characterized by hypoxic areas, herein we decided to analyze the behavior of Tc-FZ in BALB-c mice bearing mammary tumor induced with 4T1-mouse tumoral cell line. The studied ratios revealed to be slightly a little more unfavorable than in the lung tumor-porting animals, being tumor/muscle and tumor/blood ratios, at 2 h p.i., of 3.0 and 0.23, respectively. Additionally, animals in vivo images showed that the liver masked tumor signal.

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Development of fluorescent- and radio-traceable T1307-polymeric micelles as biomedical agents for cancer diagnosis: biodistribution on 4T1 tumor-bearing mice

Lecot

Rodríguez

Stancov

et al. 2022

Braz. J. Pharm. Sci.

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In recent years, nanocarriers have been studied as promising pharmaceutical tools for controlled drug-delivery, treatment-efficacy follow-up and disease imaging. Among them, X-shaped amphiphilic polymeric micelles (Tetronic®, poloxamines) display great potential due to their biocompatibility and non-toxic effects, among others. In the present work, polymeric micelles based on the T1307 copolymer were initially decorated with a 4,4-difluoro-4-bora-3a,4a-diazas-indacene (BODIPY)-fluorophore in order to determinate its in vivo biodistribution on 4T1 tumor-bearing mice. However, unfavorable results with this probe led to two different strategies. On the one hand, the BODIPY-loaded micelles, L-T1307-BODIPY, and on the other hand, the 99m Tc-radiolabeled micelles, L-T1307-99m Tc, were analyzed separately in vivo. The results indicated that T1307 accumulates mainly in the stomach, the kidneys, the lungs and the tumor, reaching the maximum organ-accumulation 2 hours after intravenous injection. Additionally, and according to the results obtained for L-T1307-99m Tc, the capture of the polymeric micelles in organs could be observed up to 24 hours after injection. The results obtained in this work were promising towards the development of new radiotracer agents for breast cancer based on X-shaped polymeric micelles.

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Preparation and Biological Evaluation of <sup>99m</sup>Tc-Labelled Phenazine Dioxides as Potential Tracers for Hypoxia Imaging

Cited by 3 publications

References 0 publications

Identification of N-Oxide-Containing Aromatic Heterocycles as Pharmacophores for Rumen Fermentation Modifiers

Identification of N-Oxide-Containing Aromatic Heterocycles as Pharmacophores for Rumen Fermentation Modifiers

<strong>99m Tc-Tricarbonyl- (2-amino- 5,10-dioxide- 7(8)-fluorophenazine) as Probe for Mammary Hypoxic-tumors Imaging</strong>

Development of fluorescent- and radio-traceable T1307-polymeric micelles as biomedical agents for cancer diagnosis: biodistribution on 4T1 tumor-bearing mice

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