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Bioorg Med Chem Lett ; 25(5): 1057-63, 2015 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-25655719

RESUMO

A new hybrid template designed by linking three pharmacophoric groups, for example, quinoline, triazole and dihydroquinoline moieties have been used for the generation of a library of molecules as potential cytotoxic agents. Synthesis of these polyazaheterocycles were carried out by using a strategy that involved one-pot sequential azidation and CuAAC in water under mild conditions. A number of 1,4-disubstituted 1,2,3-triazoles possessing quinolinylmethylene at N-1 and 1,2-dihydroquinolinyl methylene at C-4 as different substituents were synthesized and evaluated for their cytotoxic effects against various cancer cells. Some of them showed encouraging activities against lung cancer cells and one of them showed inhibition of PDE4 indicating the potential medicinal value of these novel polyazaheterocycles.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Quinolinas/química , Quinolinas/farmacologia , Triazóis/química , Triazóis/farmacologia , Antineoplásicos/síntese química , Compostos Aza/síntese química , Compostos Aza/química , Compostos Aza/farmacologia , Azidas/síntese química , Azidas/química , Linhagem Celular Tumoral , Desenho de Fármacos , Química Verde , Humanos , Simulação de Acoplamento Molecular , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia , Inibidores da Fosfodiesterase 4/síntese química , Inibidores da Fosfodiesterase 4/química , Inibidores da Fosfodiesterase 4/farmacologia , Quinolinas/síntese química , Triazóis/síntese química
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