Papers by Atilio Anzellotti
Nuclear Medicine and Biology, Oct 31, 2023
The Journal of Nuclear Medicine, May 1, 2018
Journal of Analytical & Bioanalytical Techniques, 2016
In this work, two fast and highly sensitive analytical methods, based on UV-VIS spectroscopy, wer... more In this work, two fast and highly sensitive analytical methods, based on UV-VIS spectroscopy, were adapted for its use on the determination of specific activity (SA) and Tellurium (IV) concentration, in 124 Isolutions produced by the 124 Te(p,n) 124 I reaction. The solutions analyzed showed high specific activity (209-216 Ci/mg) and Te(IV) contents below the regulatory acceptable limit (1 ppm).
Journal of Medicinal Chemistry, 2012
Eight new ruthenium complexes of clotrimazole (CTZ) with high antiparasitic activity have been sy... more Eight new ruthenium complexes of clotrimazole (CTZ) with high antiparasitic activity have been synthesized, cis,fac-[Ru II Cl 2 (DMSO) 3 (CTZ)] (1), cis,cis,trans-[Ru II Cl 2 (DMSO) 2 (CTZ) 2 ] (2), Na[Ru III Cl 4 (DMSO)(CTZ)] (3) and Na[trans-Ru III Cl 4 (CTZ) 2 ] (4), [Ru II (η 6-p-cymene)Cl 2 (CTZ)] (5), [Ru II (η 6-p-cymene)(bipy)(CTZ)][BF 4 ] 2 (6), [Ru II (η 6-p-cymene)(en)(CTZ)][BF 4 ] 2 (7) and [Ru II (η 6-p-cymene)(acac)(CTZ)][BF 4 ] (8) (bipy = bipyridine; en = ethlylenediamine; acac = acetylacetonate). The crystal structures of compounds 4-8 are described. Complexes 1-8 are active against promastigotes of Leishmania major and epimastigotes of Trypanosoma cruzi. Most notably complex 5 increases the activity of CTZ by factors of 110 and 58 against L. major and T. cruzi, with no appreciable toxicity to human osteoblasts, resulting in nanomolar and low micromolar lethal doses and therapeutic indexes of 500 and 75, respectively. In a high-content imaging assay on L. major infected intraperitoneal mice macrophages, complex 5 showed significant inhibition on the proliferation of intracellular amastigotes (IC 70 = 29 nM), while complex 8 displayed some effect at a higher concentration (IC 40 = 1 μM).
![Research paper thumbnail of A “dose on demand” Biomarker Generator for automated production of [18F]F− and [18F]FDG](https://a.academia-assets.com/images/blank-paper.jpg)
Applied Radiation and Isotopes, 2014
The University of Oklahoma-College of Pharmacy has installed the first Biomarker Generator (BG75)... more The University of Oklahoma-College of Pharmacy has installed the first Biomarker Generator (BG75) comprising a self-shielded 7.5-MeV proton beam positive ion cyclotron and an aseptic automated chemistry production and quality control module for production of [(18)F]F(-) and clinical [(18)F]FDG. Performance, reliability, and safety of the system for the production of "dose on demand" were tested over several months. No-carrier-added [(18)F]F(-) was obtained through the (18)O(p,n)(18)F nuclear reaction by irradiation (20-40 min) of a >95% enriched [(18)O]H2O target (280 μl) with a 7.5-MeV proton beam (3.5-5.0 μA). Automated quality control tests were performed on each dose. The HPLC-based analytical methods were validated against USP methods of quality control. [(18)F]FDG produced by BG75 was tested in a mouse tumor model implanted with H441 human lung adenocarcinoma cells. After initial installment and optimization, the [(18)F]F(-) production has been consistent since March 2011 with a maximum production of 400 to 450 mCi in a day. The average yield is 0.61 mCi/min and 0.92 mCi/min at 3.8 µA and 5 µA, respectively. The current target window has held up for over 25 weeks against >400 bombardment cycles. [(18)F]FDG production has been consistent since June 2012 with an average of six doses/day in an automated synthesis mode (RCY≈50%). The release criteria included USP-specified limits for pH, residual solvents (acetonitrile/ethanol), kryptofix, radiochemical purity/identity, and filter integrity test. The entire automated operation generated minimal radiation exposure hazard to the operator and environment. As expected, [(18)F]FDG produced by BG75 was found to delineate tumor volume in a mouse model of xenograft tumor. In summary, production and quality control of "[(18)F]FDG dose on demand" have been accomplished in an automated and safe manner by the first Biomarker Generator. The implementation of a cGMP quality system is under way towards the ANDA submission and first clinical use of [(18)F]FDG produced by BG75.
Introduction: In general, [18F]FDG quality assurance methods require the reporting of at least 11... more Introduction: In general, [18F]FDG quality assurance methods require the reporting of at least 11 different elements in the monograph published by the U.S. Pharmacopeia (USP). These quality tests may require the maintenance and use of as many as three different pieces of laboratory analytical equipment: Gas chromatograph, HPLC, and radio TLC. Together, this equipment adds cost of building a lab, let alone the maintenance and calibration requirements. Herein, we present an automated quality control method based upon a single HPLC system which samples 200 $mu$L radiopharmaceutical product directly from the final product vial and reports the product pH, radiochemical identity, radiochemical purity, kryptofix, FDG, acetonitrile, and ethanol concentrations. Experimental: Traditional quality control equipment were validated and used for comparison purposes. In addition the Kryptofix Color-Spot test was used as a pass fail comparison against our method. The Biomarker Generator Quality Cont...
Current Radiopharmaceuticals, 2016
Current Radiopharmaceuticals, 2016
The study aimed to develop the method of automated production on the hypoxia radiotracer 1-[18F]f... more The study aimed to develop the method of automated production on the hypoxia radiotracer 1-[18F]fluoro-3-(2-nitro-1H-imidazol-1-yl)-propan-2-ol ([18F]FMISO) on the novel fully automated platform of the BG75 system. Further validation of [18F]FMISO hypoxia imaging functionality in two tumor mouse models (FaDu/U87) was evaluated using PET/CT imaging, and the distribution of [18F]FMISO was validated by the standard hypoxia marker EF5. The average radiochemical purity was (99 ± 1) % and the average pH was 5.5 ± 0.2 with other quality attributes passing standard criteria. Overall biodistribution for [18F]FMISO in both tumor models was consistent with reported studies and high correlation was found between [18F]FMISO distribution and EF5 hypoxia staining. This study shows that qualified [18F]FMISO can be efficiently produced on the BG75 system in an automated "dose-on-demand" mode using single dose disposable cards. The possibilities of having a low-cost, automated system manufacturing ([18F]Fluoride production + synthesis + QC) different radiotracers will greatly enhance the potential for PET technology to reach new geographical areas and underserved patient populations.
Society of Nuclear Medicine Annual Meeting Abstracts, May 1, 2013
![Research paper thumbnail of Automated Manufacture of [18F]FMISO in the BG75 system. Synthesis and Purification using solid phase extraction](https://attachments.academia-assets.com/49343442/thumbnails/1.jpg)
Objectives : 1) Optimization of F-18 incorporation in 1H-imidazole-1-propanol, 2-nitro-β-[(tetrah... more Objectives : 1) Optimization of F-18 incorporation in 1H-imidazole-1-propanol, 2-nitro-β-[(tetrahydro-2H-pyran-2yl)oxy]-, 4-methylbenzenesulfonate (ester). 2) [18F]FMISO purification I. Radiochemical Purity 3) [18F]FMISO purification II. Chemical Purity 4) Automation of quality control tests for [18F]FMISO. Research Support: None Conclusions : The system BG 75 can produce doses of [18F]FMISO on demand with appropriate radiochemical yield, promising results on the automated quality controls points toward an automated production of [18F]FMISO including synthesis and purification. Results : Up to five (5) doses of sterile [18F]FMISO were produce in a single day. All key quality control requirements tested were met and the radiochemical yield for doses was in the range 30 to 40%. Proof of concept for automatization in quality control: pH, residual solvents, radiochemical identity and filter integrity tests was performed. Methods : [18F]FMISO was produced using the BG 75 system using a s...
Application of Ion Exchange HPLC towards the analysis of radiopharmaceuticals [18F]FDG and [18F]F... more Application of Ion Exchange HPLC towards the analysis of radiopharmaceuticals [18F]FDG and [18F]FMISO is shown. The results serve as proof of concept for automatization of quality control tests, required in clinical release. Radiochemical identity/purity, chemical purity and residual solvents data is presented for these radiopharmaceuticals.
Current Organic Chemistry, 2013
Acta Crystallogr E Struct Rep, 2001
... Details. Hexakis(acetonitrile)ruthenium(II) tetrachlorozincate 2.55-hydrate. Atilio Anzellott... more ... Details. Hexakis(acetonitrile)ruthenium(II) tetrachlorozincate 2.55-hydrate. Atilio Anzellotti a * and Alexander Briceño a. ... Data retrieved from the April 2001 version (5.21) of the Cambridge Structural Database (Allen & Kennard, 1993 [Allen, FH & Kennard, O. (1993). Chem. Des. ...
Inorganica Chimica Acta, Jun 1, 2006
The competitive reactions of mononucleobase cations SP-4-2-[PtCl(9-EtGua)(NH 3 )(quinoline)] + , ... more The competitive reactions of mononucleobase cations SP-4-2-[PtCl(9-EtGua)(NH 3 )(quinoline)] + , 1, and trans-[PtCl(9-EtGua)(pyridine) 2 ] + , 2, with 5 0 -guanosine monophosphate (5 0 -GMP) and N-Acetylmethionine (N-AcMet) were studied by 1 H NMR Spectroscopy. The results confirmed the previously observed kinetic selectivity for sulfur over nitrogen binding. The symmetric bis(pyridine) complex reacted faster than the ammine/quinoline moiety -the estimated half-times for reaction with 5 0 -GMP and N-AcMet were, respectively, 7.4 and 2.3 h for 1 and 4.90 and <0.75 h for 2. Thus modification of the planar amine can enhance sulfur selectivity -based on the observed rates a S/N selectivity ratio of 3.2 is obtained for 1 but >6.5 for 2. Applications of these findings were extended to study the reaction of 1 and 2 with Ubiquitin. One principal adduct corresponding to chloride displacement is observed for both species and in this case little difference in rate is observed. The likely binding site is the unique methionine residue. The percentage of platinum-bound ubiquitin is higher for 1 and 2 than the parent dichlorides trans-[PtCl 2 (NH 3 )(quinoline)] and trans-[PtCl 2 (pyridine) 2 ]. The results suggest that systematic ligand modification can modulate sulfur donor specificity and suggest possible structural features for design of platinum-based bifunctional DNA-protein cross-linking agents, rather than the DNA-DNA cross-linking principally adopted by the anticancer drug cisplatin and congeners.
Chemistry Biology, Jan 5, 2006
Noncovalent interactions are ubiquitous in ternary systems involving metal ions, DNA/RNA, and pro... more Noncovalent interactions are ubiquitous in ternary systems involving metal ions, DNA/RNA, and proteins and represent a structural motif for design of selective inhibitors of biological function. This contribution shows that small molecules containing platinated purine nucleobases mimic the natural DNA(RNA)-tryptophan recognition interaction of zinc finger peptides, specifically the C-terminal finger of HIV NCp7 protein.
Introduction: In general, [18F]FDG quality assurance methods require the reporting of at least 11... more Introduction: In general, [18F]FDG quality assurance methods require the reporting of at least 11 different elements in the monograph published by the U.S. Pharmacopeia (USP). These quality tests may require the maintenance and use of as many as three different pieces of laboratory analytical equipment: Gas chromatograph, HPLC, and radio TLC. Together, this equipment adds cost of building a lab, let alone the maintenance and calibration requirements. Herein, we present an automated quality control method based upon a single HPLC system which samples 200 $mu$L radiopharmaceutical product directly from the final product vial and reports the product pH, radiochemical identity, radiochemical purity, kryptofix, FDG, acetonitrile, and ethanol concentrations. Experimental: Traditional quality control equipment were validated and used for comparison purposes. In addition the Kryptofix Color-Spot test was used as a pass fail comparison against our method. The Biomarker Generator Quality Cont...
Journal of Radioanalytical and Nuclear Chemistry, 2015
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Papers by Atilio Anzellotti