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 |