- Chiroptical and conformational properties of (R)-1-phenylethylamine derivatives of persubstituted benzene
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Chiral derivatives of 2,4,5,6-tetrachloro-1,3-dicyanobenzene 1 with one, two and three (R)-1-phenylethylamino ((R)-PEA) units 2-4 are prepared and their chiroptical and conformational properties discussed on the bases of the UV/CD, NMR and MM2 data. High
- Kontrec, Darko,Vinkovic, Vladimir,Lesac, Andreja,Sunjic, Vitomir,Hollosi, Miklos
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- An efficient one-pot synthesis of heterocycle-fused 1,2,3-triazole derivatives as anti-cancer agents
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A series of heterocycle-fused 1,2,3-triazoles were easily prepared by the 1,3-dipolar cycloaddition of heterocyclic ketene aminals or N,O-acetals with sodium azide and polyhalo isophthalonitriles in a one-pot reaction at room temperature without a catalyst and evaluated in vitro against a panel of human tumour cell lines. 1,3-Oxazoheterocycle fused 1,2,3-triazoles were more potent against the tumour cell lines Skov-3, HL-60, A431, A549 and HepG-2 than 1,3-diazoheterocycle fused 1,2,3-triazoles. 4-Methoxyphenyl substituted 1,3-oxazoheterocycle fused 1,2,3-triazole 6j was found to be the most potent derivative with IC50 values lower than 1.9 μg/mL against A431 and K562 human tumour cell lines.
- Yan, Sheng-Jiao,Liu, Yong-Jiang,Chen, Yu-Lan,Liu, Lin,Lin, Jun
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experimental part
p. 5225 - 5228
(2010/10/01)
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