Total Synthesis-Enabled Systematic Structure–Activity Relationship Study for Development of a Bioactive Alkyne-Tagged Derivative of Neolaxiflorin L
العنوان: | Total Synthesis-Enabled Systematic Structure–Activity Relationship Study for Development of a Bioactive Alkyne-Tagged Derivative of Neolaxiflorin L |
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المؤلفون: | Lizhi Zhu, Weijian Ye, Brandon Dow Chan, Chi-Sing Lee, Magnolia Muk-Lan Lee, Mengxun Zhang, Sibao Chen, William Chi-Shing Tai, Wing Yan Wong |
المصدر: | The Journal of Organic Chemistry. 84:7007-7016 |
بيانات النشر: | American Chemical Society (ACS), 2019. |
سنة النشر: | 2019 |
مصطلحات موضوعية: | Stereochemistry, Isodon, Alkyne, Tumor cells, 010402 general chemistry, Proteomics, 01 natural sciences, Structure-Activity Relationship, chemistry.chemical_compound, Tumor Cells, Cultured, Humans, Structure–activity relationship, Cell Proliferation, chemistry.chemical_classification, Dose-Response Relationship, Drug, Molecular Structure, biology, 010405 organic chemistry, Organic Chemistry, Total synthesis, biology.organism_classification, Antineoplastic Agents, Phytogenic, Anticancer drug, 0104 chemical sciences, chemistry, Alkynes, Diterpenes, Drug Screening Assays, Antitumor, Derivative (chemistry) |
الوصف: | Neolaxiflorin L (NL) is a low-abundant Isodon 7,20-epoxy- ent-kuarenoid and was found to be a promising anticancer drug candidate in our previous study. In order to study its structure-activity relationship (SAR), a diversity-oriented synthetic route toward two libraries of (±)-NL analogs, including analogs containing different functionalities in the same 7,20-epoxy- ent-kuarene skeleton and analogs with skeletal changes, has been developed. The results of this total synthesis-enabled SAR successfully led to a bioactive alkyne-tagged NL derivative, which could be a useful probe for proteomics studies. |
تدمد: | 1520-6904 0022-3263 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1268e6d652ac7af073278bfb2301174e https://doi.org/10.1021/acs.joc.9b00748 |
حقوق: | CLOSED |
رقم الأكسشن: | edsair.doi.dedup.....1268e6d652ac7af073278bfb2301174e |
قاعدة البيانات: | OpenAIRE |
تدمد: | 15206904 00223263 |
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