With the aim of achieving new compounds possessing both anti-inflammatory and antiplatelet activities, we synthesized (E)-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides, and evaluated their COX-1 and COX-2 inhibitory and antiplatelet activities. Since COX-2 inhibitory and antiplatelet compounds have anticancer potential, we also screened their antiproliferative effects against three human cancer cell lines. Compounds 5n, 5p, 5s, 10d, 10g and 10i were determined as dual COX-2 inhibitor/antiplatelet compounds. Compound 10h appeared to be a compound that exhibited antiplatelet activity without inhibiting the COX enzyme. Compounds 5h, 10a and 10i were the most effective derivatives which displayed antiproliferative activity against Huh7, MCF7 and HCT116 cells. Particularly, compound 10i, as the compound exhibiting the highest cytotoxic, antiplatelet and COX-2 inhibitory activity, was remarkable.

中文翻译：

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作为环氧合酶抑制剂、抗血小板和抗癌剂的新型 1,3-二芳基吡唑的设计、合成和生物学评价†

为了获得具有抗炎和抗血小板活性的新化合物，我们合成了( E )-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1 H- pyrazol- 4-基]丙烯酰胺，并评估了它们的 COX-1 和 COX-2 抑制和抗血小板活性。由于 COX-2 抑制和抗血小板化合物具有抗癌潜力，我们还筛选了它们对三种人类癌细胞系的抗增殖作用。化合物5n、5p、5s、10d、10g和10i被确定为双重COX-2抑制剂/抗血小板化合物。复合10h似乎是一种在不抑制 COX 酶的情况下表现出抗血小板活性的化合物。化合物5h、10a和10i是最有效的衍生物，对Huh7、MCF7和HCT116细胞具有抗增殖活性。特别是化合物10i，作为表现出最高的细胞毒性、抗血小板和COX-2抑制活性的化合物，是显着的。