Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives
| العنوان: | Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives |
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| المؤلفون: | Silvia Marin, Marta Cascante, Daniela P.S. Alho, Jorge A. R. Salvador |
| المساهمون: | Universitat de Barcelona |
| المصدر: | Molecules Molecules, Vol 24, Iss 4, p 766 (2019) Recercat. Dipósit de la Recerca de Catalunya instname Dipòsit Digital de la UB Universidad de Barcelona Volume 24 Issue 4 |
| بيانات النشر: | MDPI, 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | pentacyclic triterpenoids, antiproliferative activity, Ketone, glycyrrhetinic acid, Stereochemistry, Cell Survival, Pharmaceutical Science, Apoptosis, Antineoplastic Agents, Chemistry Techniques, Synthetic, Conjugated system, Ring (chemistry), Jurkat cells, Article, Analytical Chemistry, lcsh:QD241-441, 03 medical and health sciences, 0302 clinical medicine, lcsh:Organic chemistry, Cell Line, Tumor, Drug Discovery, Humans, Physical and Theoretical Chemistry, Càncer, IC50, Cancer, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Molecular Structure, Organic Chemistry, Potent inducer, Cell Cycle, heterocyclic derivatives, apoptosis, Apoptosi, 3. Good health, chemistry, Chemistry (miscellaneous), Cell culture, 030220 oncology & carcinogenesis, Molecular Medicine |
| الوصف: | A new series of glycyrrhetinic acid derivatives has been synthesized via the introduction of different heterocyclic rings conjugated with an &alpha &beta unsaturated ketone in its ring A. These new compounds were screened for their antiproliferative activity in a panel of nine human cancer cell lines. Compound 10 was the most active derivative, with an IC50 of 1.1 µ M on Jurkat cells, which is 96-fold more potent than that of glycyrrhetinic acid, and was 4-fold more selective toward that cancer cell line. Further biological studies performed in Jurkat cells showed that compound 10 is a potent inducer of apoptosis that activates both the intrinsic and extrinsic pathways. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1420-3049 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1d4f7cd36b85481c291369ca33eb627Test http://europepmc.org/articles/PMC6412232Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....b1d4f7cd36b85481c291369ca33eb627 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14203049 |
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