European Journal of Medicinal Chemistry p. 836 - 842 (2015)
Update date:2022-08-15
Topics:
Lobo, Marcio M.
Viau, Cassiana M.
Dos Santos, Josiane M.
Bonacorso, Helio G.
Martins, Marcos A.P.
Amaral, Simone S.
Saffi, Jenifer
Zanatta, Nilo
Abstract The synthesis of a series of 14 new 1-(3-(aryl-4,5-dihydroisoxazol-5-yl)methyl)-4-trihalomethyl-1H-pyrimidin-2-ones from the 1,3-dipolar cycloaddition reaction of 1-allyl-4-(trihalomethyl)pyrimidin-2(1H)-ones with aryl nitrile oxides is described. Also, the antiproliferative activity of the title compounds was tested against five human tumoral cell lines: MCF-7 breast cancer cell line, ER+ (estrogen receptor positive); HepG-2 (hepatoma); T-24 (bladder cancer); HCT-116 cell (colorectal carcinoma); and CACO-2. The preliminary results are promising, since three compounds presented IC50 values below 2 μM, as well as moderate to high selectivity.
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