Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition |
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Authors: | Shen-Zhen Ren Zhong-Chang Wang Xiao-Hua Zhu Dan Zhu Zhang Li Fa-Qian Shen Yong-Tao Duan Han Cao Jing Zhao Hai-Liang Zhu |
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Affiliation: | 1. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210023, PR China;2. State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing 210023, PR China;3. Henan Provincial Key Laboratory of Children’s Genetics and Metabolic Diseases, Zhengzhou Children''s Hospital, Zhengzhou 450018, PR China |
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Abstract: | The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with chrysin. Among them, compound e9 exhibited the most potent inhibitory activity against COX-2 and antiproliferative activity against Hela cells with IC50 value of 1.12?μM. Further investigation revealed that e9 could induce apoptosis of Hela cells by mitochondrial depolarization and block the G1 phase of cell cycle in a dose-dependent manner. Besides, molecular docking simulation results was further confirmed that e9 could bind well with COX-2. In summary, compound e9 may be promising candidates for cancer therapy. |
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Keywords: | Pyrazole Chysin COX-2 inhibitor Antiproliferative Docking |
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