Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality,Challenges and Perspectives |
| |
Authors: | Débora Renz Barreto Vianna Jessica Gotardi Prof Simone Cristina Baggio Gnoatto Prof Diogo André Pilger |
| |
Affiliation: | 1. Laboratory of Biochemical and Cytological Analysis, Postgraduate Program in Pharmaceutical Sciences, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul, Avenida Ipiranga, 2752 CEP, 90610-000 Porto Alegre, Brazil;2. Laboratory of Phytochemistry and Organic Synthesis, Postgraduate Program in Pharmaceutical Sciences, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul (Brazil), Avenida Ipiranga 2752, 90610-000 Porto Alegre, Brazil |
| |
Abstract: | Chronic myeloid leukemia (CML) is a neoplasm characterized by BCR-ABL1, an oncoprotein with vital role in leukemogenesis. Its inhibition by tyrosine kinase inhibitors represents the main choice of treatment. However, therapeutic failure is worrying given the lack of pharmacological options. Pentacyclic triterpenes are phytochemicals with outstanding antitumoral properties and have also been explored as a basis for the design of potential leads. In this review, we have gathered and discuss data regarding both natural and semisynthetic pentacyclic triterpenes applied to CML cell treatment. We found consistent evidence that the class of pentacyclic triterpenes in general exerts promising pro-apoptotic and antiproliferative activities in sensitive and resistant CML cells, and thus represents a rich source for drug development. We also analyze the predicted drug-like properties of the molecules, discuss the structural changes with biological implications and show the great opportunities this class represents, as well as the perspectives they provide on drug discovery for CML treatment. |
| |
Keywords: | chronic myeloid leukemia cytotoxicity medicinal chemistry pentacyclic triterpenes phytochemistry |
|
|