| Synthesis and antitumor evaluation of neolaxiflorin B inspired compounds | |
| Liu, Jing-Ping1; Xiao, Ye-Zhi1; Hu, Yu1; Li, Xiao-Nian2; Wu, Ming-Jiang3; Zhao, Yong1; Zhao, Yan1; Ma, Ze-Jin1; Shen, Jing1 | |
| 通讯作者 | Liu, Jing-Ping(Liujp72@163.com) ; Shen, Jing(shenjingbox0225@hotmail.com) |
| 2019 | |
| 发表期刊 | DRUG DESIGN DEVELOPMENT AND THERAPY
 |
| ISSN | 1177-8881 |
| 卷号 | 13页码:3021-3028 |
| 摘要 | Background: Neolaxiflorin B is derived from ent-kaurane like laxiflorin J and eriocalyxin B with a relatively low potency as an antitumor agent. During preliminary structure-activity relationship studies, the alpha,beta-unsaturated ketone (enone) system is an important active group. Methods: Seven neolaxiflorin B derivatives containing alpha,beta-unsaturated ketone moieties were synthesized. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, and L6, respectively) by MTT assay. Results: Compound 15 appeared a promising antitumor lead due to its cytotoxic potency and relatively high selectivity, with an SI value of 13.14. Flow cytometry analysis was conducted to show that NSCLC-H292 cells were blocked in the G0/G1 phase in the presence of compound 15, thus inhibiting the proliferation of tumor cells. Conclusion: This study has revealed that compound 15 is a promising antitumor lead due to the cytotoxic potencies and the high selectivity it displayed when compared to natural counterparts. |
| 关键词 | neolaxiflorin B inspired compounds unsaturated ketone antitumor activity |
| DOI | 10.2147/DDDT.S202345 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000483086300001 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/68601 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 通讯作者 | Liu, Jing-Ping; Shen, Jing |
| 作者单位 | 1.Yunnan Normal Univ, Dept Chem, 298 121st St, Kunming 650092, Yunnan, Peoples R China 2.Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 3.Criminal Sci & Technol Key Lab Yunnan Police Coll, Kunming 650223, Yunnan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Jing-Ping,Xiao, Ye-Zhi,Hu, Yu,et al. Synthesis and antitumor evaluation of neolaxiflorin B inspired compounds[J]. DRUG DESIGN DEVELOPMENT AND THERAPY,2019,13:3021-3028. |
| APA | Liu, Jing-Ping.,Xiao, Ye-Zhi.,Hu, Yu.,Li, Xiao-Nian.,Wu, Ming-Jiang.,...&Shen, Jing.(2019).Synthesis and antitumor evaluation of neolaxiflorin B inspired compounds.DRUG DESIGN DEVELOPMENT AND THERAPY,13,3021-3028. |
| MLA | Liu, Jing-Ping,et al."Synthesis and antitumor evaluation of neolaxiflorin B inspired compounds".DRUG DESIGN DEVELOPMENT AND THERAPY 13(2019):3021-3028. |
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| Liu-2019-Synthesis a（551KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | 浏览 下载 | |
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