163596-75-6Relevant articles and documents
Synthesis and evaluation of antinociceptive and anti-inflammatory effects of nitro-porphyrins
Zapata-Morales, Juan Ramón,Pérez-González, Cuauhtémoc,Alonso-Castro, Angel Josabad,Martell-Mendoza, Miguel,Hernández-Munive, Abigail,Pérez-Gutiérrez, Salud
, p. 1782 - 1791 (2018)
This manuscript reports the anti-inflammatory and antinociceptive effects of 4 nitrophenyl-porphyrins: 5,10,15,20-tetra-(3-nitrophenyl)-porphyrin (TNPP), 5,10,15,20-tetra-(4-fluoro-3-nitrophenyl)-porphyrin (TpFNPP), 5,10,15,20-tetra-(4-chloro-3-nitrophenyl)-porphyrin (TpClNPP), and 5,10,15,20-tetra-(4-bromo-3-nitrophenyl)-porphyrin (TpBrNPP). The in vivo anti-inflammatory assays were tested on the acute and chronic TPA (12-O-tetradecanoylphorbol 13-acetate) induced ear edema. The in vitro anti-inflammatory assay was carried out using J774A.1 murine macrophages stimulated with LPS. All nitro-porphyrins decreased inflammation significantly in the acute model: 58.55% (TNPP), 67.49% (TpBrNPP), 67.49% (TpClNPP), and 71.32% (TpFNPP). TpFNPP (50 μM/ml) increased the production of the anti-inflammatory cytokine IL-10, and decreased the production of the pro-inflammatory cytokines IL-1β, TNF-α, and IL-6 in macrophages activated with LPS, with similar activity than indomethacin (50 μM/ml). All porphyrins showed antinociceptive activity and lacked visible toxicity in the acute toxicity test. These results open the possibility of further studies to determine mechanisms of action, and study the influence of the structure on the activity of such compounds.
A preparation method of the methyl two sulphur are prosperous
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Paragraph 0060; 0062-0064, (2019/07/01)
The invention relates to a preparation method of the methyl two sulphur are prosperous, to the bromobenzene formaldehyde as the starting material, the nitration reaction occurs first, then and cuprous cyanide reaction, the bromine takes on behalf of the c
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility
Sun, Lianqi,Wu, Yanbin,Liu, Yonghua,Chen, Xiaofang,Hu, Laixing
, p. 261 - 265 (2016/12/27)
The current optimization of IG-105 (3) on the carbazole-ring provided a series of new carbazole sulfonamides derivatives 13a–13m. All of the compounds have been evaluated against HepG2 cells (hepatoma cancer) for antiproliferative activity. Compounds that showed activity better or comparable to that of 3 versus HepG2 were evaluated against MCF-7 (breast cancer), MIA PaCa-2 (pancreatic cancer), and Bel-7402 (hepatoma/liver cancer) for antiproliferative activity. Of the seven compounds selected for further study five (13b, 13g, 13j, 13k and 13l) were found to give IC50values against the four cell lines comparable to those for 3. Two compounds (13f and 13i) were more active than 3 and their activity against HepG2 and MCF-7 (IC50:0.01–0.07?μM) approached that of the positive controls podophyllotoxin (podo) and CA-4. Most of compounds showed aqueous solubility (0.11–19.60?μg/mL at pH 7.4 and 2.0) better than 3. These promising results warrant further development of new compounds 13f and 13i as potential potent antitumor drug candidates.