496-72-0Relevant articles and documents
Differential antiproliferative activity of new benzimidazole-4,7-diones
Garuti, Laura,Roberti, Marinella,Pizzirani, Daniela,Pession, Annalisa,Leoncini, Emanuela,Cenci, Valentina,Hrelia, Silvana
, p. 663 - 668 (2004)
Ten benzimidazole-4,7-diones were synthesized and tested in vitro on two tumor cell lines. Several compounds showed a significant antiproliferative activity on K562 cells, although to a different extent, whereas compound 1i showed a highly significant activity on SW620 cells, comparable to that of doxorubicin. Both the substituents in the quinone ring and the position of the nitrogen atom in the pyridine moiety play a crucial role for the biological activity.
Novel cathepsin K inhibitors block osteoclasts in vitro and increase spinal bone density in zebrafish
Xue, Si-Tu,Wang, Ya-Li,Han, Xiao-Wan,Yi, Hong,Jiang, Wei,Si, Shu-Yi,Guo, Hui-Fang,Li, Zhuo-Rong
, p. 8600 - 8607 (2019/03/21)
Cathepsin K (Cat K) is a predominant cysteine protease and highly potent collagenase expressed in osteoclasts. Cat K inhibitors are anti-resorptive agents to treat osteoporosis. A novel scaffold of cathepsin K inhibitors, exemplified by lead compound 1x, was used as the template for designing and synthesizing a total of 61 derivatives that have not been reported before. An exploratory structure-activity relationship analysis identified the potent Cat K inhibitor A22, which displayed an IC50 value of 0.44 μM against Cat K. A22 was very specific for Cat K and caused a significantly higher in vitro inhibition of the enzyme as compared to that of lead compound 1x. A surface plasmon resonance analysis confirmed in vitro binding of A22 to Cat K. Molecular docking studies indicated several favourable interaction sites for A22 within the active pocket of Cat K. Furthermore, A22 also blocked active osteoclasts in vitro and increased spinal bone density in zebrafish, in which it showed an activity that was higher than that of the marketed therapeutic bone metabolizer etidronate disodium. A22 represents a very promising lead compound for the development of novel antiresorptive agents functioning as orthosteric inhibitors of Cat K.
Green synthesis and: In situ immobilization of gold nanoparticles and their application for the reduction of p -nitrophenol in continuous-flow mode
Szcs, Rózsa,Balogh-Weiser, Diána,Sánta-Bell, Evelin,Tóth-Szeles, Eszter,Varga, Tamás,Kónya, Zoltán,Poppe, László,Lagzi, István
, p. 9193 - 9197 (2019/03/28)
A green and facile method has been developed for the preparation of in situ immobilized gold nanoparticles (AuNPs) using agarose as a reducing and stabilizing agent. The size of the synthesized AuNPs ranges between 10 and 100 nm, and their average size can be controlled by the concentrations of the agarose and gold salt. The agarose matrix as a mild and green reaction medium can provide a good dispersion environment for forming AuNPs, and the hydrogel can be well homogenized with polyacrylic macroporous microbeads as well, which can adsorb and stabilize the particles leading to the simultaneous synthesis and immobilization of AuNPs avoiding harmful inorganic compounds or organic solvents. The supported gold nanocatalyst was successfully applied as a catalyst in packed bed reactors for efficient NaBH4-mediated reduction of p-nitrophenol in continuous-flow mode.