Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy
文献类型:期刊论文
作者 | Lu, Xiao-Feng1; Yang, Zheng1; Huang, Nian-Yu1; He, Hai-Bo1; Deng, Wei-Qiao2; Zou, Kun1 |
刊名 | bioorganic & medicinal chemistry letters
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出版日期 | 2015-09-01 |
卷号 | 25期号:17页码:3726-3729 |
关键词 | (25R)-Spirostan-1 Steroidal triazoles Epoxide ring-opening reaction Click chemistry Cytotoxic activities 4 6-triene-3-one |
英文摘要 | to develop more effective antitumor steroidal drugs, we synthesized a library including twenty-two novel cytotoxic 2-alkyloxyl substituted (25r)-spirostan-1,4,6-triene-3-ones and corresponding 1,2,3-triazoles through an abnormal monoepoxide ring-opening/elimination and 'click' reactions. after the cytotoxic evaluations against hepg2, caski and hela cell lines, three steroidal triazoles 5b, 5f and 5m in this library were found to possess potent anti-proliferative effects against caski cells with the half-inhibitory concentrations (ic50) of 9.4-11.8 mu m. the high-efficient and straightforward process was attractive feature for facile preparation of anti-tumor steroidal triazoles. (c) 2015 elsevier ltd. all rights reserved. |
WOS标题词 | science & technology ; life sciences & biomedicine ; physical sciences |
类目[WOS] | chemistry, medicinal ; chemistry, organic |
研究领域[WOS] | pharmacology & pharmacy ; chemistry |
关键词[WOS] | steroidal glycosides ; diosgenin ; chemistry ; saponin ; agents |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000358802900061 |
公开日期 | 2016-05-09 |
源URL | [http://cas-ir.dicp.ac.cn/handle/321008/146451] ![]() |
专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
作者单位 | 1.China Three Gorges Univ, Coll Biol & Pharmaceut Sci, Hubei Key Lab Nat Prod Res & Dev, Yichang 443002, Peoples R China 2.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian Natl Lab Clean Energy, State Key Lab Mol React Dynam, Dalian 116023, Peoples R China |
推荐引用方式 GB/T 7714 | Lu, Xiao-Feng,Yang, Zheng,Huang, Nian-Yu,et al. Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy[J]. bioorganic & medicinal chemistry letters,2015,25(17):3726-3729. |
APA | Lu, Xiao-Feng,Yang, Zheng,Huang, Nian-Yu,He, Hai-Bo,Deng, Wei-Qiao,&Zou, Kun.(2015).Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy.bioorganic & medicinal chemistry letters,25(17),3726-3729. |
MLA | Lu, Xiao-Feng,et al."Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy".bioorganic & medicinal chemistry letters 25.17(2015):3726-3729. |
入库方式: OAI收割
来源:大连化学物理研究所
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