دورية أكاديمية

Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives

التفاصيل البيبلوغرافية
العنوان: Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives
المؤلفون: Daniela P. S. Alho, Jorge A. R. Salvador, Marta Cascante, Silvia Marin
المصدر: Molecules; Volume 24; Issue 4; Pages: 766
بيانات النشر: Multidisciplinary Digital Publishing Institute
سنة النشر: 2019
المجموعة: MDPI Open Access Publishing
مصطلحات موضوعية: pentacyclic triterpenoids, glycyrrhetinic acid, heterocyclic derivatives, antiproliferative activity, apoptosis
جغرافية الموضوع: agris
الوصف: A new series of glycyrrhetinic acid derivatives has been synthesized via the introduction of different heterocyclic rings conjugated with an α,β-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 µM 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.
نوع الوثيقة: text
وصف الملف: application/pdf
اللغة: English
العلاقة: Medicinal Chemistry; https://dx.doi.org/10.3390/molecules24040766Test
DOI: 10.3390/molecules24040766
الإتاحة: https://doi.org/10.3390/molecules24040766Test
حقوق: https://creativecommons.org/licenses/by/4.0Test/
رقم الانضمام: edsbas.659F0CAA
قاعدة البيانات: BASE