Synthesis and evaluation of in vitro bioactivity for polysubstituted N-arylpyrazole derivatives |
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| Authors: | Naoto Uramaru En-Chiuan Chang Wan-Ping Yen Mou-Yung Yeh Shin-Hun Juang Fung Fuh Wong |
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| Institution: | 1. Department of Environmental Science, Nihon Pharmaceutical University, 10281, Komuro, Ina-machi, Kitaadachi-gun, Saitama, Japan;2. Department of Chemistry, National Cheng Kung University, No. 1, Ta Hsueh Rd., Tainan 70101, Taiwan, ROC;3. School of Pharmacy, China Medical University, No. 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC;4. Department of Medical Research, China Medical University Hospital, Taichung, Taiwan |
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| Abstract: | New polysubstituted N-arylpyrazole derivatives were synthesized from N1-arylsydnone with acetylene and boronic acid, including 2-thiophenyl, 3-thiophenyl, 2-benzob]thiophenyl, or dibenzothiophenyl-4-boronic acid, via 1,3-dipolar cycloaddition and Suzuki coupling reaction. Based on the growth inhibitory activity results against lung carcinoma (NCI-H226), nasopharyngeal (NPC-TW01), and T-cell leukemia (Jurkat) cancer cells, compounds 5d and 7d with dibenzothiophenyl bioisostere possessed the significant inhibitory activity for NPC-TW01 (32 μM and 16 μM) and NCI-H226 (16 μM and 8.9 μM), respectively. |
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| Keywords: | Corresponding authors at: School of Pharmacy China Medical University No 91 Hsueh-Shih Rd Taichung 40402 Taiwan ROC (F F Wong) Tel : +886 4 2205 3366x5603 fax: +886 4 2207 8083 Thiophene Benzothiophene Pyrazole Suzuki coupling reaction Bioactivity study |
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