Synthesis and cytotoxicity study of cembrane triazole derivatives

CHENG Weihua; WANG Wenqian; SHANG Hai; ZHANG Hongwu; GUO Qiang; CHEN Hong; ZOU Zhongmei

doi:10.11665/j.issn.1000-5048.20180108

Journal of China Pharmaceutical University > 2018 > 49(1): 56-63. > DOI: 10.11665/j.issn.1000-5048.20180108

CHENG Weihua, WANG Wenqian, SHANG Hai, ZHANG Hongwu, GUO Qiang, CHEN Hong, ZOU Zhongmei. Synthesis and cytotoxicity study of cembrane triazole derivatives[J]. Journal of China Pharmaceutical University, 2018, 49(1): 56-63. DOI: 10.11665/j.issn.1000-5048.20180108

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Synthesis and cytotoxicity study of cembrane triazole derivatives

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A series of triazole derivatives were designed and synthesized based on a natural product cembrane separated from Croton laevigatus Vahl which showed potential antitumor activity against HeLa cells. Twelve novel compounds were synthesized and their structures were characterized by ¹H NMR, ¹³C NMR and HRMS. Their cytotoxicities in vitro were evaluated for HeLa, K562 and K562/A02 cells by MTT assay. The results showed that some cembrane derivatives possessed antitumor activities. Substituted triazole connected to cembrane derivatives exhibited potent activity toward drug-resistant K562/A02 cells.
- cembrane,
- triazole,
- synthesis,
- structural modification,
- cytotoxicity,
- anti-drug-resistance activity

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