中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Synthesis and antitumor evaluation of neolaxiflorin B inspired compounds

文献类型:期刊论文

作者Liu, Jing-Ping3; Xiao, Ye-Zhi3; Hu, Yu3; Li, Xiao-Nian1; Wu, Ming-Jiang2; Zhao, Yong3; Zhao, Yan3; Ma, Ze-Jin3; Shen, Jing3
刊名DRUG DESIGN DEVELOPMENT AND THERAPY
出版日期2019
卷号13页码:3021-3028
ISSN号1177-8881
关键词neolaxiflorin B inspired compounds unsaturated ketone antitumor activity
DOI10.2147/DDDT.S202345
通讯作者Liu, Jing-Ping(Liujp72@163.com) ; Shen, Jing(shenjingbox0225@hotmail.com)
英文摘要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.
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000483086300001
源URL[http://ir.kib.ac.cn/handle/151853/68600]  
专题昆明植物研究所_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.Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
2.Criminal Sci & Technol Key Lab Yunnan Police Coll, Kunming 650223, Yunnan, Peoples R China
3.Yunnan Normal Univ, Dept Chem, 298 121st St, Kunming 650092, 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.

入库方式: OAI收割

来源:昆明植物研究所

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