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
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.
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.