Simulation of nonequilibrium gas flow with vibrational relaxation

Translated from Aktual'nye Voprosy Prikladnoi Matematiki, pp. 222–228, 1989.     

1-amino-2-thiobenzimidazoleimines as novel ambidentate ligand systems

Azomethine derivatives of 1-amino-2-thiobenzimidazole (H₂L) were synthesized and studied by IR and ¹H NMR spectroscopy. Thiobenzimidazoline tautomeric form of these compounds was found to predominate in a solid state and DMSO solution. Novel mono-and binuclear metal chelates M(HL)₂ and M₂L₂ (M = Ni(II), Cu(II), Co(II), Zn(II), Cd(II)) were synthesized on the basis of H₂L derivatives and their composition and structures were established from IR, ¹H NMR, EXAFS, and magnetochemical data. The composition of coordination sphere was shown to produce no effect on ferromagnetic exchange in binuclear Cu(II) complexes.     

Synthesis and Cytotoxic Activity of 4-Substituted 3-Cyano-6,6-dimethyl-5,6-dihydro-2-pyranones

The respective 4-(arylvinyl)lactones and compounds of the Michael adduct type were synthesized by the condensation of substituted benzaldehydes with 3-cyano-4,6,6-trimethyl-5,6-dihydro-2-pyranone in the presence of catalytic amounts of sodium hydroxide. It was shown by the semiempirical AM1 method that the indicated products can be formed through one and the same intermediate compound. Some of the synthesized phenylvinyl-5,6-dihydro-2-pyranones have a cytotoxic effect, and this corresponds to the prognosis of the OREX expert system.     

Synthesis of penicillin derivatives and study of their cytotoxic properties

By the interaction of heterocyclic thiols with sulfoxides of 6,6-dihydro- and 6-chloropenicillanates, derivatives of 4-heteryldithio-2-azetidinones have been synthesized, as well as products of their cyclization to form 2-heterylthiomethyl-and 2-halomethyl-substituted penicillanates and an ester of 3-chloro-3-methyl-7-chlorocepham-4-carboxylic acid. Also, the desulfurization of 6-chloropenicillanate by Raney nickel has been accomplished. For the substances that have been synthesized, a direct relationship has been established between the intensity of their cytotoxic actionin vitro with respect to tumor cells and the influence of these compounds on the intracellular generation of nitric oxide radicals.Latvian Institute of Organic Synthesis, Riga LV-1006, Translated from Khimiya Geterosiklicheskikh Soedinenii, No. 11, pp. 1494–1503, November, 1998.     

Synthesis of the first kinetically stable dibenzosilafulvene

The first stable dibenzosilafulvene, 9-{[8-(dimethylaminomethyl)-1-naphthyl]phenylsil-1-ylium}fluoren-9-ide (7a), was obtained in one step from 9-fluorenyllithium and chloro[8-(dimethylaminomethyl)-1-naphthyl]phenylsilane as a stable solvate with THF. The structure of the zwitterionic compound7a was established by¹H,¹³C, and²⁹Si NMR in solution and in the solid state. The reactions of compound7a with crotonaldehyde, ethanol, and triethylethylidenephosphorane are described. The data on the synthesis of alkoxy- and alkylthiochloro-9-fluorenylsilanes and their phosphonium salts are given. Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 3, pp. 486–491, March, 1998.     

A new method for the synthesis of silicon-and germanium-containing 2-acetylfurans and 2-acetylthiophenes

A new method was developed for the synthesis of silicon-and germanium-containing acetylfurans and acetylthiophene by metallation of 2-acetylfuran or 2-acetylthiophene with n-BuLi at low temperature after protection of the carbonyl group with lithium N-methylpiperazide and reaction of the lithium derivative with various trialkyl-, alkylphenyl-, and cycloalkylchlorosilanes or trialkylchloro(bromo)germanes. The cytotoxic activity of the new compounds was studied, and it was established that the silicon-and germanium-containing acetylfurans and acetylthiophenes are substances with low toxicity (LD₅₀ 312->2000 mg/kg) and have low cytotoxicity toward HT-1080 and MG-22A tumor cells. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 192–199, February, 2007.     

Silyl Modification of Biologically Active Compounds. 8. Trimethylsilyl Ethers of Hydroxyl-containing Thiazole Derivatives

Trimethylsilyl ethers of various hydroxyl-containing thiazole derivatives have been synthesized. The psychotropic activity (in vivo) and the cytotoxicity (in vitro on tumor cell lines HT-1080 and MG-22A) of these ethers and of their unsilylated precursors have been studied. It was discovered that the obtained compounds possess a sedative action. A moderate cytotoxic effect was detected for piperidine-containing thiazoles, displayed most strongly in relation to MG-22A cells.     

Antiviral drug Triazavirin,selectively labeled with 2H, 13C,and 15N stable isotopes. Synthesis and properties

Chemistry of Heterocyclic Compounds - Isotope-labeled antiviral drug Triazavirin containing 2H, 13C, and 15N atoms in its structure has been synthesized. 13C2H3I and KS13CN served as donors of 13C...     

Cytotoxic Activity of Ammonium Tellurates

The cytotoxic activity of a series of methylammonium tellurates on human fibrosarcoma HT-1080, mouse hepatoma MG-22A, and mouse fibroblasts 3T3 cell lines is described. The role of tellurates as free radical regulators is discussed.