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Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy
Lu, Xiao-Feng1; Yang, Zheng1; Huang, Nian-Yu1; He, Hai-Bo1; Deng, Wei-Qiao2; Zou, Kun1
KeywordSteroidal Triazoles (25r)-spirostan-1 Epoxide Ring-opening Reaction 4 Click Chemistry 6-triene-3-one Cytotoxic Activities
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2015-09-01
DOI10.1016/j.bmcl.2015.06.028
Volume25Issue:17Pages:3726-3729
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS KeywordSTEROIDAL GLYCOSIDES ; DIOSGENIN ; CHEMISTRY ; SAPONIN ; AGENTS
AbstractTo 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.
Language英语
WOS IDWOS:000358802900061
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/146451
Collection中国科学院大连化学物理研究所
Affiliation1.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
Recommended Citation
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.
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