2770-11-8Relevant articles and documents
Pd-Co catalysts prepared from palladium-doped cobalt titanate precursors for chemoselective hydrogenation of halonitroarenes
Bustamante, Tatiana M.,Dinamarca, Robinson,Torres, Cecilia C.,Pecchi, Gina,Campos, Cristian H.
, (2019/12/24)
Bimetallic Pd-Co catalysts supported on the mixed oxides CoTiO3-CoO-TiO2 (CTO) were synthesized via the thermal reduction of Pd-doped cobalt titanates PdxCo1-xTiO3 and evaluated for the chemoselective hydrogenation of halonitroarenes to haloarene-amines. The nominal Pd mass percentage of the Pd-Co/CTO systems was varied from 0.0 to 0.50. After the thermal reduction of PdxCo1-xTiO3 at 500 °C for 3 h, Pd was completely reduced and Co was partially reduced, producing a mixture of ionic Co, metallic Co, and TiO2-rutile species to give the supported bimetallic catalysts. The metallic cobalt content increased with the Pd content of the precursor. The catalytic activity toward 4-chloronitrobenzene increased with the Pd content; however, >0.1 mass% Pd decreased the chemoselectivity toward 4-chloroaniline due to the formation of the hydrodehalogenation product—aniline. The 0.1Pd-Co/CTO system was used as a model catalyst to produce haloarene-amine building blocks for linezolid, loxapine, lapatinib, and sorafenib with >98% conversion, 96% chemoselectivity, and no hydrohalogenation products. Finally, recycling tests of the 0.1Pd-Co/CTO catalyst showed loss of activity and selectivity during the third cycle due to catalyst deactivation. Regeneration treatments, every two catalytic cycles, allowed six operation cycles without loss of chemoselectivity and only a slight decrease in catalytic activity during the last cycle.
Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop
Bueno, Oskia,Gargantilla, Marta,Estévez-Gallego, Juan,Martins, Solange,Díaz, J. Fernando,Camarasa, María-José,Liekens, Sandra,Pérez-Pérez, María-Jesús,Priego, Eva-María
, p. 195 - 208 (2019/03/28)
Microtubule targeting agents represent a very active arena in the development of anticancer agents. In particular, compounds binding at the colchicine site in tubulin are being deeply studied, and the structural information recently available on this binding site allows structure-directed design of new ligands. Structural comparison of our recently reported high resolution X-Ray structure of the cyclohexanedione derivative TUB075 bound to tubulin and the tubulin-DAMA-colchicine complex has revealed a conformational change in the αT5 loop. By a grid-based computational analysis of the tubulin-DAMA-colchicine binding site, we have identified a new favourable binding area in the colchicine-site that was unexplored by our lead TUB075. Thus, based on a structure-guided design, new cyclohexanedione derivatives have been synthesized and tested for tubulin binding and in cellular assays. As a result, we have identified diphenyl ether derivatives with IC50 values around 10–40 nM against three different tumor cell lines and affinity constants for tubulin similar to that of colchicine around 107 M?1. As expected, they halted the cell cycle progression at G2/M phase at concentrations as low as 0.08 μM.
Pyrazinamide compounds and preparing method and application thereof and bactericide
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Paragraph 0141; 0142; 0144; 0146, (2019/01/14)
The invention relates to the field of pesticide bactericides, and discloses a pyrazinamide compound and a preparing method and application thereof and a bactericide. The pyrazinamide compound has thestructure shown in the formula (I) or the formula (II) or the formula (III). According to the pyrazinamide compound and the preparing method and application thereof and the bactericide, by introducingpyrazine ring fragments and and diphenyl ether fragments with the wide biological activity in NNF-0721, and the pyrazinamide compound with the brand-new structure is designed; the pyrazinamide compound can serve as a brand-new succinodehydrogenase inhibitor or a bactericide. The formula is defined in the description.
