13019-32-4Relevant articles and documents
Chemoselective synthesis of 5-amino-7-bromoquinolin-8-yl sulfonate derivatives and their antimicrobial evaluation
Krishna, Palaa
, p. 685 - 690 (2018)
A series of new 5-amino-7-bromoquinolin-8-ol sulfonate derivatives 5(a–j) were synthesized from 8-hydroxyquinoline through multi-step process with high yields using mild, efficient and conventional methods. Chemoselectivity was observed during the transfo
SMALL MOLECULES TARGETING MUTANT MAMMALIAN PROTEINS
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Paragraph 0188; 0189, (2021/10/02)
Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with a mutation in a protein.
A SAR study: Evaluation of bromo derivatives of 8-substituted quinolines as novel anticancer agents
?kten, Salih,?akmak, Osman,Tekin, ?aban,K?prülü, Tu?ba Kul
, p. 1415 - 1424 (2017/12/28)
Background: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5, 7-Dibromo- 5, 7-bromo- 6, 7-cyano- 11 and 5, 7-dicyano-12 8-hydroxyquinolines were shown to have strong antiproliferative activity against various tumor cell lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) with IC50 values ranged from 6.7 to 25.6 μg/mL. Methods: A structure activity relationship (SAR) was conducted that quinoline core containing hydroxly group at C-8 positon led to more anti cancer potentials. Results: The results of Lactate Dehydrogenase (LDH) cytotoxic, DNA laddering and inhibition assays indicated that 5, 6, 11 and 12 have high cytotoxic effects and appototic potentials. Conclusion: Furthermore, 5 and 12 have inhibitory effects on relaxation of supercoiled plazmid DNA by supressed the Topoisomerase I enzyme. As a result, 5, 6, 11 and 12 may have promising anticancer drug potential and 5 and 12 may be novel topoisomerase inhibitors.
A new method of bromination of aromatic rings by an iso-amyl nitrite/HBr system
Gavara, Laurent,Boisse, Thomas,Rigo, Beno?t,Hénichart, Jean-Pierre
, p. 4999 - 5004 (2008/09/21)
A mixture of iso-amyl nitrite/HBr is shown to be a mild and efficient reagent for electrophilic aromatic bromination. The reaction succeeds with slightly activated arenes and heterocyclic compounds. By using HCl instead of HBr, chlorination can also be performed in few cases. The i-amONO2/HBr mixture can also be utilized for bromination in the α-position of electron withdrawing groups. A possible mechanism is briefly discussed.
Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
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Page/Page column 40 - 41, (2010/02/10)
Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Ortho-Specific Bromination of Phenols
Schmitz, Ernst,Pagenkopf, Ingeborg
, p. 998 - 1006 (2007/10/02)
Phenol as well as 3-substituted phenols are brominated exclusively in the ortho positions by N.N-dibromomethylamine, yielding 2.6-dibrominated phenols in excellent yields.Phenols bearing an ortho-substituent need N-bromomethylamine as the brominating agent to take up one bromine atom into the free ortho-position. para-Bromination is not observed in either case. 1-Naphthol gives 2-bromo-1-naphthol, 8-hydroxyquinoline gives 7-bromo-8-hydroxyquinoline with 80percent and 98percent yield respectively. ortho-Specific chlorination of phenols was carried out in some cases using N-chloro-alkylamines.
