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- W2036610614 abstract "This Letter reports the synthesis and biological evaluation of a collection of aminophthalazines as a novel class of compounds capable of reducing production of PGE2 in HCA-7 human adenocarcinoma cells. A total of 28 analogs were synthesized, assayed for PGE2 reduction, and selected active compounds were evaluated for inhibitory activity against COX-2 in a cell free assay. Compound 2xxiv (R1 = H, R2 = p-CH3O) exhibited the most potent activity in cells (EC50 = 0.02 μM) and minimal inhibition of COX-2 activity (3% at 5 μM). Furthermore, the anti-tumor activity of analog 2vii was analyzed in xenograft mouse models exhibiting good anti-cancer activity." @default.
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- W2036610614 date "2013-01-01" @default.
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- W2036610614 title "Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE2 production in cells" @default.
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- W2036610614 doi "https://doi.org/10.1016/j.bmcl.2012.11.030" @default.
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