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
Corresponding AuthorLiu, Jing-Ping( ; Shen, Jing(
AbstractBackground: 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.
Keywordneolaxiflorin B inspired compounds unsaturated ketone antitumor activity
Indexed BySCI
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS IDWOS:000483086300001
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Document Type期刊论文
Corresponding AuthorLiu, Jing-Ping; Shen, Jing
Affiliation1.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
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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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