Synthesis and anticancer activity of 4-aza-daurinol derivatives
| العنوان: | Synthesis and anticancer activity of 4-aza-daurinol derivatives |
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| المؤلفون: | Ju-Yeun Lee, Dongyun Shin, Sung Jean Park, Nam-Song Choi, Faisal Hayat, Seung-Hyuk Park |
| المصدر: | Archives of Pharmacal Research. 38:1975-1982 |
| بيانات النشر: | Springer Science and Business Media LLC, 2015. |
| سنة النشر: | 2015 |
| مصطلحات موضوعية: | chemistry.chemical_classification, Chemistry, Stereochemistry, Aryl, Organic Chemistry, Pharmacology toxicology, Antineoplastic Agents, Naphthalenes, Combinatorial chemistry, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Cell culture, Cell Line, Tumor, Neoplasms, Drug Discovery, Humans, Molecular Medicine, Structure–activity relationship, Benzodioxoles, Cancer cell lines, Lactone, Cell Proliferation |
| الوصف: | Daurinol, a natural aryl naphthalene lactone, has been reported to have antiproliferative activity against various cell lines, and has also been shown to be efficacious in an in vivo xenograft mouse model. In this study, we tried to discover a new scaffold that enables both rapid structure-activity relationship study of daurinol and scalable synthesis of active compounds. 4-Aza-daurinol, a bioisosterism-based scaffold of daurinol, was designed and 17 analogues were synthesized and evaluated against five representative cancer cell lines. Among them, the 2,3-dihydrobenzo[b][1,4]dioxinyl derivative was found to be the most potent and showed similar activity and tendency as daurinol. |
| تدمد: | 1976-3786 0253-6269 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23d58d7916168ea31369a45ed44bf66f https://doi.org/10.1007/s12272-015-0619-2 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....23d58d7916168ea31369a45ed44bf66f |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 19763786 02536269 |
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