Novel 5‐Methyl‐2‐[(un)substituted phenyl]‐4‐{4,5‐dihydro‐ 3‐[(un)substituted phenyl]‐5‐(1,2,3,4‐tetrahydroisoquinoline‐2‐yl)pyrazol‐1‐yl}‐oxazole Derivatives: Synthesis and Anticancer Activity |
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| Authors: | Xinhua Liu Linshan Bai Chunxiu Pan Baoan Song Hailiang Zhu |
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| Institution: | 1. Anhui Key Laboratory of Coal Clean Conversion and Utilization, School of Chemistry and Chemical Engineering, Anhui University of Technology, Maanshan, Anhui 243002, China;2. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, Jiangsu 210093, China |
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| Abstract: | Eleven novel 5‐methyl‐2‐(un)substituted phenyl]‐4‐{4,5‐dihydro‐3‐(un)substituted phenyl]‐5‐(1,2,3,4‐tetrahydroisoquinoline‐2‐yl)pyrazol‐1‐yl}‐oxazole derivatives were synthesized and characterized by elemental analysis, ESI‐MS, 1H NMR and 13C NMR. All of the compounds have been screened for their antiproliferative activities against PC‐3 cell (human prostate cancer) and A431 cell (human epidermoid carcinoma cancer) lines in vitro. The results revealed that compounds 4g , 4j and 4k exhibited the strong inhibitory activities against the PC‐3 cell lines (with IC50 values of 2.8±0.11, 3.1±0.10 and 3.0±0.06 μg/mL, respectively). |
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| Keywords: | synthesis aryl‐dihydropyrazole 1 2 3 4‐tetrahydroisoquinoline anticancer activity |
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