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KMID : 0043320150380050791
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Archives of Pharmacal Research
2015 Volume.38 No. 5 p.791 ~ p.800
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Discovery and synthesis of novel allylthioaralkylthiopyridazines: their antiproliferative activity against MCF-7 and Hep3B cells
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Park Hae-Sun
Kim Chae-Won
Park Myung-Sook
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Abstract
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A new series of 6-allylthio-3-aralkylthio-4,5-dimethylpyridazines 5a?5k and 1-allylthio-4-alkylthio-5,6,7,8-tetrahydrophthalazine 6a?6j was synthesized frommaleic anhydride derivatives for development of newanticancer agents. The process involves the formation ofpyridazine and phthalazine rings, dichlorination, allylthiolation,and aralkylthiolation. These new compoundsshowed antiproliferative activities against breast cancer(MCF-7) and hepatocarcinoma (Hep3B) cells in CCK-8assays, and could be promising candidates for chemotherapyof carcinomas. Among 21 synthesized compounds, fivecompounds (5a, 5b, 6b, 6d, and 6f) showed higher potencythan 5-FU for inhibiting the growth of cell line. The resultsindicated that compound 6f had the highest activitytowards MCF-7 and Hep3B cells. These results suggest thepotential anticancer activity of compounds 5a, 5b, 6b, 6d,and 6f.
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KEYWORD
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Organosulfur compounds, 4, 5-Dimethylpyridazines, Tetrahydrophthalazins, Antiproliferative, MCF-7/Hep3B cells
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