Photoinitiated azo-hydrazo tautomerizm of 1- p

A novel photochromic compound with NH-N intramolecular H-bond (1-p-toluenesulphonylazo- 2,4,6,8-tetrakis(tert-butyl)phenoxazine) and the corresponding model structures (1-oxo-2,4,6,8-tetrakis(tertbutyl) phenoxazine, 2,4,5,7-tetrakis (tert-butyl )-1-( veratroylazo ) phenoxazine, 2,4,5,7-tetrakis ( tert-butyl )-Nacetyl- 1-(p-toluenesulphonylazo)phenoxazine) have been synthesized and their spectral and photochemical properties are studied. The photochromic transformations observed are found to be conditioned by ESIPT (as a primary step) followed by E-Z isomerisation about N–N-bond

Acylated 2-(N-arylaminomethylene)benzo[b]thiophene-3(2H)-Ones: Molecular Switches with Varying Migrants and Substituents

Synthesis and properties of photochromic acylated 2-(N-arylaminomethylene)benzo[b]thiophene-3(2H)-ones are described. Their structure largely depends on the nature of acyl migrant and in a less degree on N-aryl substituent

Elication of an excitation center in the depth of tissue by visualization with high-frequency electric field

Hardware and software system, which makes it possible to visualize the glow center, marker of the excitation center in tissue, in the electric field, is created. The system was tested in 14 experiments with sinoatrial nodes of cat's hearts, which's fist excitation's center is in the depth of the right auricle's myocardium, and in 30 experiments with frog's venous sinuses, which's first excitation's center is situated in the superficial layer of the sinus wall. Also observations were held with deeply situated center - in cat's tooth's pulp, which is surrounded by insulators: dentine and tooth's enamel. The ability of visualization the excitation's center was developed at localizations in different depths

Synthesis of Novel Iono- and Photochromic Spiropyrans Derived from 6,7-Dihydroxy-8-Formyl-4-Methyl-2H-Chromene-2-One

Novel photochromic spiropyrans (SPPs) containing 6′-hydroxy group were synthesized and their spectral properties as well as abilities for complexation with metal ions studied. In solutions they exist as equilibrium mixture of spirocyclic (A) and merocyanine (B) isomers. The largest content of merocyanine form was found for the derivative with an electron-donating methyl group in position 5 of hetaryl fragment. The irradiation of SPPs in acetonitrile shifts the equilibrium to the B form. Similar effect causes the addition of metal cations due to formation of colored complexes with merocyanine isomers

Structural Conformers of (1,3-Dithiol-2-ylidene)ethanethioamides: The Balance Between Thioamide Rotation and Preservation of Classical Sulfur-Sulfur Hypervalent Bonds

The reaction of N-(2-phthalimidoethyl)-N-alkylisopropylamines and S2Cl2 gave 4-N-(2-phthalimidoethyl)-N-alkylamino-5-chloro-1,2-dithiol-3-thiones that quantitatively cycloadded to dimethyl or diethyl acetylenedicarboxylate to give stable thioacid chlorides, which in turn reacted with one equivalent of aniline or a thiole to give thioanilides or a dithioester. Several compounds of this series showed atropisomers that were studied by a combination of dynamic NMR, simulation of the signals, conformational analysis by DFT methods, and single crystal X-ray diffraction, showing a good correlation between the theoretical calculations, the experimental values of energies, and the preferred conformations in the solid state. The steric hindering of the crowded substitution at the central amine group was found to be the reason for the presence of permanent atropisomers in this series of compounds and the cause of a unique disposition of the thioxo group at close-to-right angles with respect to the plane defined by the 1,3-dithiole ring in the dithiafulvene derivatives, thus breaking the sulfur–sulfur hypervalent bond that is always found in this kind of compounds.Ministerio de Economıá y Competitividad, Spain (Project CTQ2012- 31611), Junta de Castilla y León, Consejería de Educación y Cultura y Fondo Social Europeo (Project BU246A12-1), and the European Commission, Seventh Framework Programme (Project SNIFFER FP7-SEC-2012-312411

Vascular endothelial growth factor acts as an osteolytic factor in breast cancer metastases to bone

Vascular endothelial growth factor (VEGF) is a proangiogenic cytokine that is expressed highly in many solid tumours often correlating with a poor prognosis. In this study, we investigated the expression of VEGF and its receptors in bone metastases from primary human breast tumours and further characterised its effects on osteoclasts in vitro. Breast cancer metastases to bone were immunohistochemically stained for VEGF, its receptors VEGFR1 and 2 (vascular endothelial growth factor receptor 1 and 2), demonstrating that breast cancer metastases express VEGF strongly and that surrounding osteoclasts express both VEGFR1 and VEGFR2. RAW 264.7 cells (mouse monocyte cell line) and human peripheral blood mononuclear cells (PBMCs) were cultured with VEGF, RANKL and M-CSF. VEGF and RANKL together induced differentiation of multinucleated, tartrate-resistant acid phophatase (TRAP)-positive cells in similar numbers to M-CSF and RANKL. The PBMCs were also able to significantly stimulate resorption of mineralised matrix after treatment with M-CSF with RANKL and VEGF with RANKL. We have shown that VEGF in the presence of RANKL supports PBMC differentiation into osteoclast-like cells, able to resorb substrate. Vascular endothelial growth factor may therefore play a role in physiological bone resorption and in pathological situations. Consequently, VEGF signalling may be a therapeutic target for osteoclast inhibition in conditions such as tumour osteolysis

Malignant melanoma and bone resorption

The cellular and humoral mechanisms accounting for osteolysis in skeletal metastases of malignant melanoma are uncertain. Osteoclasts, the specialised multinucleated cells that carry out bone resorption, are derived from monocyte/macrophage precursors. We isolated tumour-associated macrophages (TAMs) from metastatic (lymph node/skin) melanomas and cultured them in the presence and absence of osteoclastogenic cytokines and growth factors. The effect of tumour-derived fibroblasts and melanoma cells on osteoclast formation and resorption was also analysed. Melanoma TAMs (CD14+/CD51−) differentiated into osteoclasts (CD14−/CD51+) in the presence of receptor activator for nuclear factor κB ligand (RANKL) and macrophage-colony stimulating factor. Tumour-associated macrophage-osteoclast differentiation also occurred via a RANKL-independent pathway when TAMs were cultured with tumour necrosis factor-α and interleukin (IL)-1α. RT–PCR showed that fibroblasts isolated from metastatic melanomas expressed RANKL messenger RNA and the conditioned medium of cultured melanoma fibroblasts was found to be capable of inducing osteoclast formation in the absence of RANKL; this effect was inhibited by the addition of osteoprotegerin (OPG). We also found that cultured human SK-Mel-29 melanoma cells produce a soluble factor that induces osteoclast differentiation; this effect was not inhibited by OPG. Our findings indicate that TAMs in metastatic melanomas can differentiate into osteoclasts and that melanoma fibroblasts and melanoma tumour cells can induce osteoclast formation by RANKL-dependent and RANKL-independent mechanisms, respectively

КЛИНИЧЕСКИЕ РЕКОМЕНДАЦИИ. ДИАГНОСТИКА И ЛЕЧЕНИЕ РАКА РОТОГЛОТКИ

Клинические рекомендации подготовлены на основании материалов научно-практической конференции Проблемной комиссии «Опухоли головы и шеи» Научного совета по злокачественным новообразованиям Отделения медицинских наук Российской академии наук и Министерства здравоохранения РФ, посвященной памяти профессора Александра Ильича Пачеса, «Актуальные вопросы диагностики и лечения рака ротоглотки» (25 июня 2015 г., г. Архангельск).Клинические рекомендации подготовлены на основании материалов научно-практической конференции Проблемной комиссии «Опухоли головы и шеи» Научного совета по злокачественным новообразованиям Отделения медицинских наук Российской академии наук и Министерства здравоохранения РФ, посвященной памяти профессора Александра Ильича Пачеса, «Актуальные вопросы диагностики и лечения рака ротоглотки» (25 июня 2015 г., г. Архангельск)