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Evaluation of new naphthalimides as potential anticancer agents against breast cancer MCF-7, pancreatic cancer BxPC-3 and colon cancer HCT- 15 cell lines

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Detalhes bibliográficos
Resumo:New 1,8-naphthalimido derivatives with 2,3 and 4 carbon chains bearing a number of different functionalities were synthesized and tested against a panel of breast cancer MCF-7, colon cancer HCT-15 and pancreatic cancer BxPC-3 cell lines. Generally structures with shorter alkyl chains were more active, with the one exception of the amide containing a p-nitrophenyl group. GI50 values (µM) were determined for the most active compounds. Three compounds exhibited GI50 values below 5 µM, two with MCF-7 cells, and one other with HCT-15. Compounds with different functionalities demonstrated cell line specificity: the MCF-7 cell line was more sensitive to an urea derivative (6f), the growth of HCT15 cells were most affected by a triazole (9d), while the BxPC-3 cell line was inhibited in a higher extend by a guanidine (4a).
Autores principais:Noro, Jennifer Martins
Outros Autores:Maciel, J.; Duarte, D.; Olival, A. C. D.; Baptista, C.; Silva, A. C. D.; Alves, Maria José Chão; Kong, Thoo Lin
Assunto:Toxicity Tetrabromide Naphthalimide Isocyanate Membrane permeabilization Ciências Naturais::Ciências Químicas
Ano:2015
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso restrito
Instituição associada:Universidade do Minho
Idioma:inglês
Origem:RepositóriUM - Universidade do Minho
Descrição
Resumo:New 1,8-naphthalimido derivatives with 2,3 and 4 carbon chains bearing a number of different functionalities were synthesized and tested against a panel of breast cancer MCF-7, colon cancer HCT-15 and pancreatic cancer BxPC-3 cell lines. Generally structures with shorter alkyl chains were more active, with the one exception of the amide containing a p-nitrophenyl group. GI50 values (µM) were determined for the most active compounds. Three compounds exhibited GI50 values below 5 µM, two with MCF-7 cells, and one other with HCT-15. Compounds with different functionalities demonstrated cell line specificity: the MCF-7 cell line was more sensitive to an urea derivative (6f), the growth of HCT15 cells were most affected by a triazole (9d), while the BxPC-3 cell line was inhibited in a higher extend by a guanidine (4a).