CP*RUOM~)~, (2), (Cp* = qS-C5Me5) has been prepared from ( C ~* R U C I ~) ~, (I), in MeOH and converted to (CP*RUCI)~, (3), in pentane with Me,SiCI; both complexes (2) and (3) readily react to give Cp*RuL2X complexes on addition of the appropriate ligands L.Since the discovery of ( c p * R ~C l ~) ~t in 19841 several groups24 have exploited the synthetic potential of this material for the synthesis of organometallic, in particular Cp*Ru complexes (Cp* = C5Me5). Co-ordinatively unsaturated Ru" species should be able to play a key role since they -t Note udded in proof: recent X-ray structure determinations have disclosed ( I ) and (2) to be dirneric (U. Koelle, R. Boese, N. Klaff, and G. H. Herberich. to be published) and (3) to be a tetrarner in the solid
2,6 ]undec-8-ene-3,5-dione. -The compounds (I) and (II) are completely inactive towards bacteria and fungi and do not show any activity against HIV-1. (IIa) does not protect from clonic seizures and tonic convulsions evoked by pentetrazole. -(STRUGA*, M.; KOSSAKOWSKI, J.; KEDZIERSKA, E.; FIDECKA, S.; STEFANSKA, J.; Chem. Pharm. Bull. 55 (2007) 5, 796-799; Dep. Med. Chem., Med. Univ., PL-02-007 Warsaw, Pol.; Eng.) -K. Woydowski 45-198
A large group of aminoalkyl and aminoalkanol derivatives of selected dicarboximides were synthesized and characterized by 1HNMR, 13CNMR and ESI MS spectra analysis. The thirty nine new compounds were tested for their cytotoxic properties in human chronic (K562), acute leukemia (HL-60), and cervical cancer cells (HeLa) as well as in normal endothelial cells (HUVEC). The most promising compounds are 4-[2-(dimethylamino)ethyl]-, (diethylamino) ethyl]-, 4-[2-(piperidin-1-yl)ethyl]-, 4-[3-(dimethylamino)propyl]- and 4-[2-hydroxy-3-(propan- 2-ylamino)propyl]- derivatives of 1,7-diethyl-8,9-diphenyl-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5,10-trione exhibiting high and selective cytotoxicity towards K562 and HL-60 cells (IC50 in the range of 1-10 µM) while being non-toxic towards HUVEC and HeLa cells (IC50> 100 μM). Moreover, the preliminary studies have showed that 4-[2-(piperidin-1-yl)ethyl]- 1,7-diethyl-8,9-diphenyl-4-azatricyclo [5.2.1.0(2,6)]dec-8-ene-3,5,10-trione induces programmed cell death (apoptosis) in leukemia cells.
Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. 1H-NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive bacteria (MIC 50 to 200 μg/mL). Compounds VI and III exhibited antifungal activity against the Candida strains C. albicans and C. parapsilosis (MIC – 100 μg/mL).
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