- Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety
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A series of novel bisquinoline derivatives connected by a 4-oxy-3-fluoroaniline moiety were synthesized and evaluated for their in vitro antitumour activities against a panel of five cancer cell lines (H460, HT-29, MKN-45, U87MG, and SMMC-7721). Most of compounds tested showed a potent activity and high selectivity towards the H460 and MKN-45 cell lines. Among the compounds tested, six (15d, 15e, 15m, 15n, 16a, and 16i) were further examined for their c-Met kinase activity; the compounds showed high efficacy with IC 50 values in the single-digit nM range. An analysis of structure-activity relationships indicated that an unsubstituted or a halogen-substituted phenyl ring on the 2-arylquinoline-4-carboxamide moiety was favourable for antitumour activity.
- Li, Sai,Huang, Qiang,Liu, Yajing,Zhang, Xiaolong,Liu, Shuang,He, Chao,Gong, Ping
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- NOVEL PHENYL-QUINOLINE-CARBOXYLIC ACID PYRIDINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
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This invention relates to novel phenyl-quinoline-carboxylic acid pyridine derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the tre
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Page/Page column 7
(2011/09/16)
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- NOVEL PHENYL-QUINOLINE-CARBOXYLIC ACID PYRIDINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
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This invention relates to novel phenyl-quinoline-carboxylic acid pyridine derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the tre
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Page/Page column 15
(2010/04/03)
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- A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase
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A series of quinoline inhibitors of C. albicans prolyl tRNA synthetase was identified. The most potent analogue, 2-(4bromo-phenyl)-6-chloro-8-methyl-4-quinolinecarboxylic acid, showed IC50=5 nM (Ca. ProRS) with high selectivity over the human enzyme.
- Yu, Xiang Y.,Hill, Jason M.,Yu, Guixue,Yang, Yifeng,Kluge, Arthur F.,Keith, Dennis,Finn, John,Gallant, Paul,Silverman, Jared,Lim, Audrey
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p. 541 - 544
(2007/10/03)
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- Synthesis and aldose reductase inhibitory activity of N-(quinolinyl thiocarbonyl) glycine derivatives
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The onset of diabetic complications may be prevented by the inhibition of aldose reductase.Derivatives of N-(quinolinyl thiocarbonyl) glycine were prepared and their in vitro and ex vivo aldose reductase inhibitory activities were tested on rat lens.The cincophen derivatives were the most potent in vitro with an enzyme inhibition value of 29percent at 10-8 M and 91percent at 10-7 for the N--N-methylglycine compound 10a.This activity was shown to be dependent on the nature of the substituents and seems to be optimal for the acids; esterswerefound to be inactive.No compound have shown ex vivo inhibitory activity.It is concluded that the lack of ex vivo activity is likely due to a poor bioavailability or a bad penetration of the compounds in target tissue (lens). aldose reductase inhibitors / diabetic complications / N-(quinolinyl thiocarbonyl) glycine
- Nicolaie, E,Guengoer, T,Goyard, J,Cure, G,Fouquet, A,et al.
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p. 977 - 984
(2007/10/02)
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