[en] Biologically active indole derivative was synthesized and screened for its cytotoxicity against breast cancer cell line (MCF-7) with the IC₅₀ equals 17.5 µg/mL. Docking study showed its high binding affinity to the COX-2 enzyme. It's radiolabeling with ^99mTc and showed high radiochemical yield (92.10 ± 0.57%) and in vitro stability in serum up to 10 h. Biodistribution studies of a novel ^99mTc-NSIC complex in tumor-bearing mice showed high T/NT ratio (6.17 ± 0.08 at 30 min. post-injection), suggesting this complex could be used as a solid tumor imaging agent. (author)

[en] Various concentrations of HCl or HNO₃ on Zirconium Vanadate (ZrV) gel as an ion exchanger were studied by batch technique to determine the K_d values of ⁴⁷Ca(II) and ⁴⁷Sc(III) ions. A small chromatographic column packed with ZrV gel for ⁴⁷Sc(III) separation based on a high elution yield with high purity from the point of view chemical, radiochemical and radionuclidic. The maximum elution yield of ⁴⁷Sc (88 ± 2.2%) was obtained using 60% acetone-0.2 M HCl as an eluent. The ⁴⁷Sc was separated with acceptable radionuclidic purity (> 99.98±0.001%) and radiochemical purity (99. 0.09%), in addition to a very low concentrations of Ca⁺² ( 0.05 ppm) which is lower than the permissible level (10 ppm) for medical applications, particularly for the labelling of pharmaceutical compounds

[en] A novel sulphonamide derivative (EPBS) was prepared at high yield and characterized by ¹H NMR and infrared radiation spectroscopy. Its cytotoxic activity was examined in breast carcinoma (MCF-7) cells at a dose of 25 μg/mL. Approximately 68 percent effective inhibition has been achieved. Furthermore, the synthesized ligand was directly radiolabeled with technetium-99m using sodium borohydride. High radiochemical purities (95.5%) were determined using radio-paper chromatography and electrophoresis. Its in vivo evaluation in tumor bearing mice demonstrated a high tumor uptake of the ^99mTc-EPBS complex at 30 min post injection (6.74%) and tumor/muscle (T/NT) ratio equal to 5.04 ± 0.05. In conclusion, ^99mTc-EPBS agent showed favorable characteristics for the radio-diagnosis of solid tumors. (author)

[en] Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and "1H NMR spectroscopy. It was radiolabeled with iodine-131 by direct electrophilic substitution reaction and radiochemical yield was determined by using different chromatographic techniques (HPLRC, paper chromatography and paper electrophoresis). "1"3"1I-HPZPHT has high radiolabeling yield (98.00 ± 2.00 %), stability, solid tumor uptake and T/NT ratio (5.17 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer. (author)

[en] A new dipeptide derivative, ethyl 2-(3-(4-hydroxyphenyl)-2-(2-(4-phenyl-5-((pyridin-4-ylamino)methyl)-4H-1,2, 4-triazol-3-ylthio)acetamido)propanamido)-3-(1H-indol-3-yl)propanoate (EHPTIP) was successfully synthesized and radiolabeled with ¹²⁵I by the direct electrophilic substitution method. The non radiolabeled compound (EHPTIP) was tested as an antimicrobial agent and the radiolabeled derivative was tested as a new imaging agent. The study results showed a good antimicrobial activity of EHPTIP and a good in vitro and in vivo stability of ¹²⁵I-EHPTIP. The biodistribution of the radiolabeled compound showed a high brain uptake of 7.60 ± 0.01 injected activity/g tissue organ at 30 min post-injection and retention in brain remained high up to 1 h, whereas the clearance from the normal mice appeared to proceed via the renal system. Such brain uptake is better than that of currently used radiopharmaceuticals for brain imaging (^99mTc-ECD and ^99mTc-HMPAO). As a conclusion, EHPTIP is a newly synthesized dipeptide with a good antimicrobial activity and the radioiodinated EHPTIP which is labeled with ¹²³I could be used as a novel agent for brain SPECT. (author)

[en] This work spotlights on the rapid and effective separation method for the no-carrier-added (NCA) ⁴⁷Sc from natural irradiated Ti target using an anionic exchanger resin; AN-31 impregnated with 4-(2-Pyridylazo) resorcinol (PAR). The newly prepared resin (An-PAR) was characterized by FTIR and SEM. The Influence of pH on the distribution coefficients (K_d) of Sc(III) and Ti(IV) ions was investigated by batch technique and the results revealed that Ti(IV) ions are strongly adsorbed by AN-PAR rather than AN-31, while Sc(III) ions are weakly adsorbed on the both resin materials. The radiochemical separation of ⁴⁷Sc(III) from irradiated natural Ti target was successfully carried out, where the elution efficiency for ⁴⁷Sc reached 89 ± 1.5% with high radiochemical, radionuclidic and chemical purities. Our findings thus hold a great promise for the use of ⁴⁷Sc radioisotope in the preparation of radiopharmaceuticals for theranostics applications. (author)

[en] Using a one-pot cyclo-condensation process under microwave irradiation, derivatives of curcumin have been created. Evaluation their anti-inflammatory efficacy showed that they had stronger properties than curcumin. Additionally, the most active derivative was radiolabeled with the diagnostic radioisotope technetium-99m and prepared with a high radiochemical yield (96.5 ± 0.09%) and in vitro stability of up to 6 h. The in-vivo study in inflamed mice showed that [^99mTc]Tc-curcumin derivative accumulated with a high target to non-target ratio. The gathered information confirmed the efficacy of the [^99mTc]Tc-curcumin derivative as a novel possible tracer for the identification and localization of inflammation. (author)

[en] Thidiazuron (TDZ) was reported to possess anti-cancer activity against Human cervical carcinoma cell line, so that this study has been conducted for the radiolabeling of TDZ with Technetium-99m. The conditions of the radiolabeling process were optimized and a high radiochemical yield of 93.1 ± 0.35% has been obtained. Molecular docking study illustrated that [^99mTc]technetium bisthiadiazuron (^99mTc-TDZ) complex has the ability to bind with Caspase-3 protein that over expressed in cancers. Its in-vivo biodistribution on solid tumor bearing mice showed comparatively high T/NT ratio of 6.87 ± 0.14 at 60 min post injection. These promising characteristics make our new designed labeled conjugate a very suitable candidate for molecular imaging of solid tumors, particularly in the cervix. (author)

[en] Feasibility of ¹⁹⁹Au production from neutron activated platinum and gold targets at the Egyptian Second Research Reactor was studied. A comparison between theoretical calculations and experimental measurements for the two targets was carried out. A radiochemical separation of ¹⁹⁹Au from irradiated Pt target was achieved using chromatographic column packed with modified chabazite material with elution efficiency of 90 ± 0.54% based on the high separation factor between Au and other produced undesired radionuclides. Three quality control tests; radionuclidic, radiochemical and chemical purities were carried out on the eluted ¹⁹⁹Au to ensure its safe application in nuclear medicine. (author)

[en] Highlights: • Poly (acrylamide-acrylic Acid)/multi-walled carbon nanotubes composite was prepared by gamma radiation to initiate the copolymerization of AAm and AA onto MWCNTs surface. • Separation factors (Sc-47/Ca-47) based on distribution coefficient data suggested that nitric acid is distinctly better medium as compared to hydrochloric acid. • Radiochemical separation of ⁴⁷Sc(III) from ⁴⁷Ca(II) showed that HNO₃ is a better medium for complete retention and recovery of ⁴⁷Sc(III). • The eluted ⁴⁷Sc radionuclides were of high radiochemical, radionuclidic and chemical purity. - Abstract: Poly (acrylamide-acrylic Acid)/multi-walled carbon nanotubes composite [P(AAm-AA)/MWCNTs] was prepared by gamma radiation to initiate the copolymerization of AAm and AA onto MWCNTs surface. The structural characteristics were confirmed by FT-IR, SEM, XRD, TGA and DTA. The particle size distribution was determined by dynamic light scattering (DLS). [P(AAm-AA)/MWCNTs] was used to study the adsorption efficiency of ⁴⁷Sc from natural calcium by batch technique at different concentrations of HCl and/or HNO₃ acid solutions. No-carrier-added ⁴⁷Sc (III) was separated from ⁴⁷Ca(II) on [P(AAm-AA)/MWCNTs] column matrix. The elution efficiency of about 80 ± 1.5% was attained for ⁴⁷Sc(III) using 1M HNO₃. Three quality control tests, radionuclidic, radiochemical and chemical purities were investigated to emphasis that ⁴⁷Sc secure for use in nuclear medicine.