Molecular design of multitarget neuroprotectors 2. Synthesis and bioactivity of carbazole—γ-carboline conjugates

Russian Chemical Bulletin - Earlier unknown conjugates of carbazoles and γ-carbolines were obtained by the reaction of 3,6-substituted 9-oxiranylmethylcarbazoles and 2,8-substituted...     

Bis(4-nitrobenzenethiolato)tetranitrosyldiiron: synthesis,structure, and pharmacological activity of a new nitric oxide (NO) donor

Russian Chemical Bulletin - A preparative procedure was developed for the synthesis of new binuclear tetranitrosyl iron complex of the “μ-S” structural type, [Fe2(SC6H4NO2)2(NO)4]...     

Adamantane acid esters with alkoxyaryl alcohols: Synthesis,antiproliferative activity,and influence on microtubule network of tumor cells

Adamantaneacetic and adamantanecarboxylic acid esters containing 3-hydroxy-4-methoxybenzyl, 3,4,5-trimethoxybenzyl, or 5-(hydroxymethyl)-2-methoxyphenyl groups were synthesized as unusual analogs of natural antitumor and anti-tubulin agents combretastatin A-4 and 2-methoxyestradiol. The compounds were found to possess noticeable cytotoxicity to epithelial human carcinoma cell line A549 (EC₅₀ = 4.3—81 μmol L^–1). An ability to cause complete depolymerization of microtubule network of A549 cells was demonstrated for 5-(hydroxymethyl)-2-methoxyphenyl adamantan-1-ylacetate (6a) at a concentration of 100 μmol L^–1. Ester 6a belongs to a new structural type, which is unusual for the ligands of the tubulin colchicine domain, and is an interesting lead compound for further structural optimization.     

Ferrocene-containing tri- and tetranuclear cyclic copper(<Emphasis Type="SmallCaps">i</Emphasis>) and silver(<Emphasis Type="SmallCaps">i</Emphasis>) pyrazolates

New tri- and tetranuclear macrocyclic silver(i) and copper(i) 3-ferrocenyl-5-(trifluoromethyl)pyrazolates were prepared: [{(3-((η⁵-C₅H₄)Fe(η⁵-C₅H₅))-5-(CF₃)-Pz}M]₃ (M = Cu (1), Ag (2)) and [{(3-(( η⁵-C₅H₄)Fe(η⁵-C₅H₅))-5-(CF₃)-Pz}Cu]₄ (3). The structures of compounds were established by X-ray diffraction analysis. In the crystalline state, a planar trinuclear silver-containing macrocycliс pyrazolate and a saddle-shaped tetranuclear copper-containing macrocycle are formed. The introduction of a bulky substituent, ferrocene, into the pyrazole ligand results in complete shielding of the acidic metal sites, which precludes the coordination of base molecules.     

Synthesis of furyl-, furylvinyl-, thienyl-, pyrrolinylquinazolines and isoindolo[2,1-<Emphasis Type="Italic">a</Emphasis>]quinazolines

A method for the synthesis of hydrogenated furyl-, furylvinyl-, thienyl-, and pyrrolinyl-substituted quinazolin-4-ones was developed. A possibility of the reaction of 2-furylquinazolines with maleic anhydride was demonstrated. A number of quinazolines obtained were subjected to a primary bioscreening on inhibition of acetylcholinesterase.     

Synthesis of trinuclear Cu<Superscript>II</Superscript>-complex with tris(4-triphenylmethylphenoxy)-substituted hemihexaphyrazine and radioprotective properties of its water-soluble form

A condensation of 2,5-diamino-1,3,4-thiadiazole with the products of the in situ reaction of 1,2-dicyano-4-(4-triphenylmethylphenoxy)benzene with sodium alkoxides in a mixture of butanol—methanol furnished a trisubstituted ABABAB-type macroheterocycle (hemihexaphyrazine). A 3 : 1 trinuclear complex was synthesized by the reaction of the macrocycle with copper(II) acetate. The compounds obtained were characterized by IR spectroscopy, UV-vis spectroscopy, mass spectrometry, as well as by elemental analysis. Radioprotective properties of the water-soluble form of the complex were studied     

Complexes of organotin compounds with bis- and trisphosphonate derivatives of 2,6-di-tert-butylphenol having antioxidant activity

Russian Chemical Bulletin - Complexes of organotin compounds R2SnCl2 with bisand trisphosphonate derivatives of 2,6-di-tert-butyl-4-methylphenol (ionol) were synthesized. X-ray diffraction studies...     

Synthesis of methylene-bis(1-oxy-3,3-dialkyl-1-triazene 2-oxides) and their analogs

Synthetic procedures towards methylene-bis(1-oxy-3,3-dialkyl-1-triazene 2-oxides), the first representatives of a new class of promising exogenous nitric oxide (NO) donors, which can release NO in living organisms, were developed. Synthesis involves the reactions of salts of 1-hydroxy-3,3-dialkyl-1-triazene 2-oxides with either dibromomethane or 1-chloromethoxy-3,3-dialkyl-1-triazene 2-oxides.     

Coordination compounds of DyIII and NdIII with malonic and succinic acid bispicolylamidrazones

Russian Chemical Bulletin - Dysprosium(iii) and neodymium(iii) complexes with aliphatic dicarboxylic acid bispicolyl-amidrazones were synthesized and studied. X-ray diffraction data showed that the...