排序方式: 共有43条查询结果,搜索用时 15 毫秒
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Luca G. Iacovino Luca Pinzi Giorgio Facchetti Beatrice Bortolini Michael S. Christodoulou Claudia Binda Giulio Rastelli Isabella Rimoldi Daniele Passarella Maria Luisa Di Paolo Lisa Dalla Via 《ACS medicinal chemistry letters》2021,12(7):1151
A library of monosubstituted chalcones (1–17) bearing electron-donating and electron-withdrawing groups on both aromatic rings were selected. The cell viability on human tumor cell lines was evaluated first. The compounds unable to induce detectable cytotoxicity (1, 13, and 14) were tested using the monoamine oxidase (MAO) activity assay. Interestingly, they inhibit MAO-B, acting as competitive inhibitors, with 13 and 14 showing the best profiles. In particular, 13 exhibited a potency higher than that of safinamide, taken as a reference. Docking studies and crystallographic analysis showed that in human MAO-B 13 binds with the halogen-substituted aromatic ring in the entrance cavity, similar to safinamide, whereas 14 is accommodated in the opposite way. The main conclusion of this cell biology, biochemistry, and structural study is to highlights 13 as a chalcone derivative that is worth consideration for the development of novel MAO-B-selective inhibitors for the treatment of neurodegenerative diseases. 相似文献
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Insuasty B Chamizo L Muñoz J Tigreros A Quiroga J Abonía R Nogueras M Cobo J 《Archiv der Pharmazie》2012,345(4):275-286
Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. The in vitro antitumor activity of the obtained compounds was determined at the National Cancer Institute (NCI). The 5-(benzo[d][1,3]dioxol-5-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (9a) is the most prominent of the compounds due to its remarkable activity toward leukemia (RPMI-8226), renal cancer (UO-31) and prostate cancer (DU-145) cell lines with GI(50) values of 1.88, 1.91 and 1.94 μM, respectively. 相似文献
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