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Jo, Nam Hyun,Kim, Jung Young,El‐,Gamal, Mohammed I.,Choi, Won‐,Kyoung,Park, Jin‐,Hun,Kim, Eun Jung,Cho, Jung‐,Hyuck,Ha, Hyun‐,Joon,Choi, Tae Hyun,Oh, Chang‐,Hyun John Wiley Sons, Ltd. 2011 Journal of labelled compounds & radiopharmaceutica Vol.54 No.2
<P><B>Abstract</B></P><P>Synthesis, radiolabelling, and <I>in vitro</I> evaluation of a new <SUP>125</SUP>I‐labelled iodouracil hexitol nucleoside analogue are reported. The target compound was successfully synthesized by an iodination–destannylation method and then purified by reverse phase HPLC. The radiochemical purity of the product was >99% with decay‐corrected yields of 48±3%. <I>In vitro</I> cellular uptake testing was carried out using MCA and MCA‐tk cell lines for comparison of compound 1 with [<SUP>18</SUP>F]FHBG. The newly synthesized compound 1 showed higher accumulation in herpex simplex virus type 1 thymidine kinase (HSV1‐tk) gene expression cell line (MCA‐tk cell line) than in the wild type MCA cell line compared with [<SUP>18</SUP>F]FHBG. The MCA‐tk to MCA cellular uptake ratio for compound 1 was higher than that of [<SUP>18</SUP>F]FHBG from 2 h after incubation. The radioiodine‐labelled compound 1 (I‐125, <I>t</I><SUB>1/2</SUB>=59.37 days) has a longer physical half‐life than F‐18‐(<I>t</I><SUB>1/2</SUB>=110 min) labelled FHBG. Radioiodine‐labelled compound 1 could be used for monitoring gene expression for a long time. The selectivity for MCA‐tk cell line makes compound 1 a promising imaging agent for HSV1‐tk expression. Copyright © 2010 John Wiley & Sons, Ltd.</P>
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Khedr, Abdalla M.,Gaber, Mohamed,Abd El‐,Zaher, Eman H. SCIENCE PRESS 2011 CHINESE JOURNAL OF CHEMISTRY Vol.29 No.6
<P><B>Abstract</B></P><P>The synthesis and characterization of new transition metal complexes of Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) with 3‐(2‐hydroxynaph‐1‐ylazo)‐1,2,4‐triazole (<B>HL<SUP>1</SUP></B>) and 3‐(2‐hydroxy‐3‐carboxynaph‐1‐ylazo)‐1,2,4‐triazole (<B>HL<SUP>2</SUP></B>) have been carried out. Their structures were confirmed by elemental analyses, thermal analyses, spectral and magnetic data. The IR and <SUP>1</SUP>H NMR spectra indicated that <B>HL<SUP>1</SUP></B> and <B>HL<SUP>2</SUP></B> coordinated to the metal ions as bidentate monobasic ligands via the hydroxyl O and azo N atoms. The UV‐Vis, ESR spectra and magnetic moment data revealed the formation of octahedral complexes [Mn<B>L<SUP>1</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>3</SUB>] (<B>1</B>), [Co<B>L<SUP>1</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>3</SUB>]·H<SUB>2</SUB>O (<B>2</B>), [Mn<B>L<SUP>2</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>3</SUB>] (<B>6</B>) and [Co<B>L<SUP>2</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>3</SUB>] (<B>7</B>), [Ni<B>L<SUP>1</SUP></B>(AcO)(H<SUB>2</SUB>O)] (<B>3</B>), [Zn<B>L<SUP>1</SUP></B>(AcO)(H<SUB>2</SUB>O)]·H<SUB>2</SUB>O (<B>5</B>), [Ni<B>L<SUP>2</SUP></B>(AcO)(H<SUB>2</SUB>O)] (<B>8</B>), [Zn<B>L<SUP>2</SUP></B>(AcO)(H<SUB>2</SUB>O)]·10H<SUB>2</SUB>O (<B>10</B>) have tetrahedral geometry, whereas [Cu<B>L<SUP>1</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>2</SUB>] (<B>4</B>) and [Cu<B>L<SUP>2</SUP></B>(AcO)(H<SUB>2</SUB>O)<SUB>2</SUB>]·5H<SUB>2</SUB>O (<B>9</B>) have square pyramidal geometry.. The mass spectra of the complexes under EI‐con‐ ditions showed the highest peaks corresponding to their molecular weights, based on the atomic weights of <SUP>55</SUP>Mn, <SUP>59</SUP>Co, <SUP>58</SUP>Ni, <SUP>63</SUP>Cu and <SUP>64</SUP>Zn isotopes; besides, other peaks containing other isotopes distribution of the metal. Kinetic and thermodynamic parameters of the thermal decomposition stages were computed from the thermal data using Coats‐Redfern method. <B>HL<SUP>2</SUP></B> and complexes <B>6</B>–<B>10</B> were found to have moderate antimicrobial activities against <I>Staphylococcus aureus </I>(gram positive), <I>Escherichia coli </I>(gram negative) and <I>Salmonella </I>sp bacteria, and antifungal activity against <I>Fusarium oxysporum</I>, <I>Aspergillus niger</I> and <I>Candida albicans</I>. Also, in most cases, metallation increased the activity compared with the free ligand.</P>
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