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ANTI-TUMOR POTENTIAL OF 4-AMINO-2-ARYL-6,9-DICHLOROBENZO[G]PTERIDINES
Autores:
VIOLETA CARMONA MARTÍNEZ
,
ANTONIO JOSÉ RUIZ ALCARAZ
, ANTONIO GUIRADO,
MARÍA CONCEPCIÓN MARTÍNEZ-ESPARZA ALVARGONZÁLEZ
,
MARIA PILAR GARCÍA PEÑARRUBIA
,
Grupos de investigación:
[GI/IMIB/C063/2011] Inmunidad innata en la salud y la enfermedad
Comunicación:
Antecedentes:
Pteridines are bicyclic heterocyclic compounds based on pyrimidine rings. Derivatives from this chemical structure core family have shown many therapeutic utilities. Concretely, 4-aminopteridine derivates have demonstrated both anti-inflammatory and anti-cancer properties, and some of them, such as methotrexate, are profusely used in medical practice. In particular, methotrexate, also called MTX, was first used as part of combined chemotherapies to treat different types of cancer, and for the last 30 years it has been used as well as a therapeutic agent to treat several autoimmune diseases, including among others rheumatoid arthritis and severe psoriasis. Other interesting pteridine derivatives are 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines, whose biological activity has been poorly studied. We had recently synthesized and tested the biological activity of a series of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines. We found that this series present anti-inflammatory properties, since they were able to inhibit in vitro the production of pro-inflammatory cytokines TNF-? and IL-6.
Métodos:
We have evaluated the anti-tumor potential of these compounds by using leukemia cell lines HL-60 cells (ATCC® CCL-240™), derived from a human myeloid leukemia, and K562 cells (ATCC® CCL-243™), lymphoblasts derived from chronic myelogenous leukemia. Cells growing at exponential rate were exposed to decreasing doses of each compound, from 50 to 0.3 ?M, for 24, 48 and 72 hours. Then cells viability was tested by MTT assays. A total of 16 pteridine derivatives were analyzed.
Resultados:
Among the compounds that showed cytotoxic activity, 7j and 7k were active against both HL-60 and K562 cells, having a lower IC50 when tested on HL-60 cells. Compounds 7a, 7b and 7g had a great cytotoxic activity against HL-60, but they were far less potent against K562 cells. Compounds 6c and 7d were also active when exposed to HL-60 cells, but they did not exceed 60% cytotoxicity with the highest doses.
Conclusiones:
Our results demonstrate that some compounds of this series of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines have potent anti-cancer properties in vitro.
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