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Investigations in the 99mTc chemistry are stimulated by the search for new radiopharmaceuticals for nuclear medical applications. To understand the coordination mode of Tc with various complexing agents, macroscopic studies of technetium coordination chemistry are often performed using the low energy ß-emitting radionuclide 99Tc, which has a much longer half life (t1/2 = 2.12 x 105 years) than 99mTc, in the mg level. Investigations of Re coordination chemistry are done in conjunction with Tc studies because Re possesses chemical properties similar to those of Tc. For some chemical tasks, Re provides a non-radioactive alternative to work with Tc radioisotopes. In addition, 186Re and 188Re are of great interest to nuclear medicine as they possess nuclear properties favorable for use in therapeutic radiopharmaceuticals. Our investigations of Tc and Re coordination chemistry are toward this goal. A large series of technetium and rhenium complexes resulted from this studies have been characterized by X-ray crystal structure determinations. This survey covers the structural investigations performed by P.Leibnitz and G.Reck (BAM) from 1992 till now. It summarizes results obtained in the Rossendorf technetium group and is not intended to compete with the well-written reviews published so far.

Investigations in the 99mTc chemistry are stimulated by the search for new radiopharmaceuticals for nuclear medical applications. To understand the coordination mode of Tc with various complexing agents, macroscopic studies of technetium coordination chemistry are often performed using the low energy ß-emitting radionuclide 99Tc, which has a much longer half life (t1/2 = 2.12 x 105 years) than 99mTc, in the mg level. Investigations of Re coordination chemistry are done in conjunction with Tc studies because Re possesses chemical properties similar to those of Tc. For some chemical tasks, Re provides a non-radioactive alternative to work with Tc radioisotopes. In addition, 186Re and 188Re are of great interest to nuclear medicine as they possess nuclear properties favorable for use in therapeutic radiopharmaceuticals. Our investigations of Tc and Re coordination chemistry are toward this goal. A large series of technetium and rhenium complexes resulted from this studies have been characterized by X-ray crystal structure determinations. This survey covers the structural investigations performed by P.Leibnitz and G.Reck (BAM) from 1992 till now. It summarizes results obtained in the Rossendorf technetium group and is not intended to compete with the well-written reviews published so far.

This work is dedicated to thorough structural analysis of plant bifunctional nuclease TBN1, the representative of plant nuclease I group. TBN1 along with homologous nucleases from this family plays an important role in plant cell life cycle and also shows considerable anticancerogenic effects. Two variants of TBN1 (wild type and N211D mutant) were studied. Properties of both variants in different solutions were analyzed. Both were successfully crystallized. Structures of both types of TBN1 were solved using X-ray diffraction. The phase problem was solved by Multi-wavelength anomalous dispersion using Zn2+ ions natively present in TBN1. Structural properties of TBN1 such as fold, active site composition, effect of glycosylation and surface electrostatic potential distribution were analyzed. Reaction mechanism of TBN1 was proposed on the basis of structural properties and comparisons with similar structures.

京都大学 / 0048 / 新制・課程博士 / 博士(工学) / 甲第21129号 / 工博第4493号 / 新制||工||1698(附属図書館) / 京都大学大学院工学研究科化学工学専攻 / (主査)教授 宮原 稔, 教授 山本 量一, 教授 佐野 紀彰 / 学位規則第4条第1項該当 / Doctor of Philosophy (Engineering) / Kyoto University / DFAM

<p>Opisane&nbsp; su&nbsp; sinteze&nbsp; novih&nbsp; liganada&nbsp; bis(ftalazin-1hidrazon)-2,6-diacetilpiridna&nbsp; (Hz₂DAP&middot;2HCl),&nbsp; bis(3-hlorpiridazin-6-hidrazon)-2,6-diacetilpiridina (Hp₂DAP),&nbsp; 3-hlorpiridazin-6-hidrazon&nbsp; di(2-piridil) ketona&nbsp; (HpDPK),&nbsp; ftalazin-1-hidrazon&nbsp; di(2-piridil)<br />ketona&nbsp; (HzDPK)&nbsp; i&nbsp; ftalazin-1-hidrazon&nbsp; piridin-2-karbaldehida&nbsp; (HzPY).&nbsp; Zajedničko&nbsp; svojstvo&nbsp; dobijenih liganada&nbsp; je&nbsp; &scaron;to&nbsp; sadrže&nbsp; piridinski&nbsp; i&nbsp; diazinski&nbsp; prsten&nbsp; i sadrže&nbsp; samo&nbsp; donorne&nbsp; atome&nbsp; azota.&nbsp; Tokom&nbsp; nastajanja kompleksa dolazi do deprotonacije liganada. Svi ligandi su&nbsp; okarakterisani&nbsp; elementalnom&nbsp; analizom, termoanalitičkim&nbsp; metodama&nbsp; i&nbsp; metodom&nbsp; IR spektroskopije,&nbsp; dok&nbsp; neki&nbsp; i&nbsp; metodom&nbsp; NMR spektroskopije&nbsp; kao&nbsp; i&nbsp; rendgenskom&nbsp; strukturnom analizom.Za&nbsp; sintezu&nbsp; koordinacionih&nbsp; jedinjenja&nbsp; primenjeni&nbsp; soli Co(II),&nbsp; Ni(II),&nbsp; Cu(II)&nbsp; i&nbsp; Zn(II).&nbsp; Dobijeni&nbsp; kompleksi su okarakterisani&nbsp; elementalnom&nbsp; analizom, konduktomerijskim&nbsp; i&nbsp; magnetnim&nbsp; merenjima,&nbsp; IR spektroskopijom i termoanalitičkim metodama. Barem jedan&nbsp; kompleks&nbsp; iz&nbsp; svake&nbsp; serije&nbsp; je&nbsp; okarakterisan&nbsp; i rendgenskom strukturnom analizom. Urađena&nbsp; su&nbsp; i&nbsp; ispitivanja&nbsp; antimikrobne&nbsp; aktivnosti odabranih&nbsp; jedinjenja&nbsp; prema&nbsp; predstavnicima&nbsp; grampozitivnih i gram-negativnih bakterija i kulturu kvasca. Pored&nbsp; toga,&nbsp; urađena&nbsp; su&nbsp; i&nbsp; ispitivanja&nbsp; citotoksične,antiproliferativne&nbsp; i&nbsp; inhibitorne&nbsp; aktivnosti&nbsp; jedinjenja prema&nbsp; roditeljskim&nbsp; i&nbsp; multirezistentnim&nbsp; T-limfomnim ćelijama&nbsp; kancera.&nbsp; Utvrđeno&nbsp; je&nbsp; da&nbsp; neka&nbsp; jedinjenja pokazuju&nbsp; izrazito&nbsp; mikrobicidno,&nbsp; citotoksično, antiproliferativno i inhibitorno dejstvo.</p> / <p>The synthesis of new ligands dihydrochloride salt of 2,6-diacetylpyridne&nbsp;&nbsp; bis(phthalazine-1hydrazone) (Hz₂DAP&bull;2HCl),&nbsp; 2,6-diacetylpiridine&nbsp; bis(3- chloropyridazine-6-hydrazone)&nbsp; (Hp₂DAP),&nbsp; di(2-pyridyl)ketone&nbsp; 3-chloropyridazine- 6-hydrazone (HpDPK),&nbsp; di(2-pyridyl)ketone&nbsp; phthalazine-1-hydrazone&nbsp; (HzDPK)&nbsp; and&nbsp; &nbsp; pyridine-2-carbaldehide phthalazine-1-hydrazone&nbsp; (HzPY)&nbsp; have&nbsp; been described. All the ligands contain pyridine and diazine core and all of them have only nitrogen donor atoms. During the complex formation the deprotonation of ligands takes&nbsp; places.&nbsp; All&nbsp; of&nbsp; the&nbsp; ligands&nbsp; have&nbsp; been characterized&nbsp; by&nbsp; elemental&nbsp; analysis,thermoanalytical&nbsp; methods&nbsp; and&nbsp; IR&nbsp; spectroscopy.&nbsp; In some&nbsp; cases&nbsp; also&nbsp; by&nbsp; NMR&nbsp; spectroscopy&nbsp; and&nbsp; X-ray structural analysis.Co(II), Ni(II), Cu(II) and Zn(II) salts were&nbsp; used for the synthesis&nbsp; of&nbsp; the&nbsp; coordinational&nbsp; compounds.&nbsp; The obtained complexes were characterized by elemental analysis,&nbsp; molar&nbsp; conductivity&nbsp; and&nbsp; magnetic measurements,&nbsp; IR&nbsp; spectroscopy&nbsp; and thermoanalytical&nbsp; methods.&nbsp; At&nbsp; least&nbsp; one complex&nbsp; of each&nbsp; series&nbsp; were&nbsp; characterized&nbsp; by&nbsp; X-ray&nbsp; structural analysis.The antimicrobial activity of some of the compounds toward&nbsp; Gram-positive/Gram- negative&nbsp; bacteria furthermore,&nbsp; the&nbsp; cytotoxic,&nbsp; antiproliferative&nbsp; and inhibitory&nbsp; activity&nbsp; toward&nbsp; sensitive&nbsp; parental&nbsp; andmultiresistant&nbsp; T-lymphoma&nbsp; cancer&nbsp; cells&nbsp; have&nbsp; also been carried out. It&nbsp; can&nbsp; be&nbsp; concluded&nbsp; that&nbsp; some&nbsp; of&nbsp; the&nbsp; compounds exhibit&nbsp; outstanding&nbsp; antimicrobial,&nbsp; cytotoxic, antiproliferative, and inhibitory activity.</p>