Caged Garcinia Xanthones: Synthetic Studies and Pharmacophore Evaluation
| Autor: | Oraphin Chantarasriwong, Nicholas J. Checchia, Bashayer D. Althufairi, Emmanuel A. Theodorakis |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Bioactive scaffold biology 010405 organic chemistry Stereochemistry biology.organism_classification 01 natural sciences 0104 chemical sciences Human tumor 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology chemistry Xanthone Gambogic acid Pharmacophore Garcinia |
| DOI: | 10.1016/b978-0-444-64056-7.00004-0 |
| Popis: | The Garcinia genus of plants has yielded an intriguing family of caged xanthone-derived natural products that have a documented value in traditional Eastern medicine. Collectively referred to as caged Garcinia xanthones (CGXs), these compounds are defined by an unusual motif in which the C-ring of an allylated xanthone has been converted into a tricyclic cage. This motif is further decorated via A-ring substitutions and peripheral oxidations to produce a variety of related subfamilies. Gambogic acid, the archetype of this family, has shown efficacy in several human tumor xenograft models and has entered clinical trials in China for the treatment of cancer. Its promising therapeutic potential has fueled the evolution of synthetic strategies, aiming to synthesize various natural products of this family and optimize its bioactive scaffold. This review will present the general chemical concepts that have been explored toward the synthesis of CGX natural products and will discuss how they have been applied for the study of the CGX pharmacophore. |
| Databáze: | OpenAIRE |
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