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Bioorg Med Chem Lett ; 25(11): 2360-5, 2015 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-25933593

RESUMO

PMA-SiO2 catalyzed Pictet-Spengler reaction of aryl amine linked to C-3 of the indole and the aryl aldehydes was achieved. In the series of the synthesized compounds, 6b, 10b and 12b were found to be cytotoxic against prostate, lung, breast and cervical cancer cell lines selectively with no significant effect on the growth of the control fibroblast cell line NIH3T3. Further determining their cytotoxic potential we found that 10b and 12b show cell cycle arrest in DU145 prostate cancer cells indicating a role in cell cycle progression. Both the molecules showed effect on decreased phosphorylation of NF-κB on serine 536 residue which is strongly implicated in many different types of cancers. Taken together, the series of indoloquinolines elicit potent anti-cancer potential providing a mean for developing novel indoloquinoline based anti-cancer agents.


Assuntos
Antineoplásicos/farmacologia , Fosforilcolina/análogos & derivados , Ácidos Polimetacrílicos/química , Quinolinas/síntese química , Quinolinas/farmacologia , Dióxido de Silício/química , Antineoplásicos/química , Linhagem Celular Tumoral , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Fosforilcolina/química , Relação Estrutura-Atividade
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