6623-41-2Relevant articles and documents
Synthetic method of aminophenol compounds
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Paragraph 0097-0101; 0152-0154, (2020/08/09)
The invention provides a synthesis method of aminophenol compounds. The synthesis method comprises the following steps: taking an carbon-coated nickel nano composite material containing alkaline-earthmetals as a catalyst, and catalyzing a hydrogenation reduction reaction of nitro-phenol compounds in a hydrogen atmosphere; wherein the nano composite material contains a core-shell structure with ashell layer and an inner core, the shell layer is a graphitized carbon layer containing alkaline-earth metals and oxygen, and the inner core is nickel nano particles. According to the method, the nanocomposite material is used as a catalyst; a carbon material and the nickel nano particles generate a synergistic effect and a good catalytic effect, the alkaline-earth metals of the shell layer further synergistically improve the catalytic performance of the nano composite material, and the catalyst is used for hydrogenation reduction of nitro-phenol compounds to synthesize aminophenol compounds,and has excellent activity, selectivity and safety.
Antitumor agents. 5. Synthesis, structure - activity relationships, and biological evaluation of dimethyl-5H-pyridophenoxazin-5-ones, tetrahydro-5H-benzopyridophenoxazin-5-ones, and 5H-benzopyridophenoxazin-5-ones with potent antiproliferative activity
Bolognese, Adele,Correale, Gaetano,Manfra, Michele,Lavecchia, Antonio,Novellino, Ettore,Pepe, Stefano
, p. 5110 - 5118 (2007/10/03)
New antiproliferative compounds, dimethyl-5H-pyrido[3,2-a]phenoxazin-5-ones (1-6), tetrahydro-5H-benzopyrido[2,3-j]phenoxazin-5-ones (7-9), and 5H-benzopyrido[3,2-a]phenoxazin-5-ones (10-12) were synthesized and evaluated against representative human neoplastic cell lines. Dimethyl derivatives 1-6 were more active against carcinoma than leukemia cell lines. The tetrahydrobenzo derivatives 7-9 were scarcely active, whereas the corresponding benzo derivatives 10-12 showed notable cytotoxicity against a majority of the tested cell lines. Molecular modeling studies indicated that the high potency of 10 and 11, the most cytotoxic compounds of the whole series, could be due to the position of the condensed benzene ring, which favors π-π stacking interactions with purine and pyrimidine bases in the DNA active site. Biological studies suggested that 10-12 have no effect on human topoisomerases I and II and that they induce arrest at the G2/M phase.
Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut
Sato, Yasuo,Yamada, Megumi,Yoshida, Satoshi,Soneda, Tomoko,Ishikawa, Midori,Nizato, Tetsutaro,Suzuki, Kokichi,Konno, Fukio
, p. 3015 - 3021 (2007/10/03)
A series of benzoxazoles with a nitrogen-containing heterocyclic substituent at the 2-position was prepared and evaluated for 5-HT3 partial agonist activity on isolated guinea pig ileum. The nature of the substituent at the 5-position of the benzoxazole ring affected the potency for the 5-HTs receptor, and the 5-chloro derivatives showed increased potency and lowered intrinsic activity. 5-Chloro-7-methyl-2-(4-methyl-1- homopiperazinyl)benzoxazole (6v) exhibited a high binding affinity in the same range as that of the 5-HT3 antagonist granisetron, and its intrinsic activity was 12% of that of 5-HT. Compound 6v inhibited 5-HT-evoked diarrhea but did not prolong the transition time of glass beads in the normal distal colon even at a dose of 100 times the ED50 for diarrhea inhibition in mice. Compounds of this type are expected to be effective for the treatment of irritable bowel syndrome without the side effect of constipation.
