Discovery of Novel Bioactive Tanshinones and Carnosol Analogues against Breast Cancer
[EN] The abietane diterpenoids ferruginol (1), tanshinone IIA (3), and carnosol (4) are well-known for their interesting pharmacological properties, including antitumor, similar to other natural and semisynthetic abietanes. In this study, a pair of semisynthetic C18-functionalized analogues of 3 and...
| Authors: | , , , |
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| Format: | article |
| Publication Date: | 2023 |
| Country: | España |
| Institution: | Universitat Politècnica de València (UPV) |
| Repository: | RiuNet. Repositorio Institucional de la Universitat Politécnica de Valéncia |
| Language: | English |
| OAI Identifier: | oai:riunet.upv.es:10251/203878 |
| Online Access: | https://riunet.upv.es/handle/10251/203878 |
| Access Level: | Open access |
| Keyword: | Breast cancer Abietane Dehydroabietylamine Catechol Ortho-quinone Phthalimide 03.- Garantizar una vida saludable y promover el bienestar para todos y todas en todas las edades |
| Summary: | [EN] The abietane diterpenoids ferruginol (1), tanshinone IIA (3), and carnosol (4) are well-known for their interesting pharmacological properties, including antitumor, similar to other natural and semisynthetic abietanes. In this study, a pair of semisynthetic C18-functionalized analogues of 3 and 4 were prepared from the commercially available (+)-dehydroabietylamine or readily obtained methyl dehydroabietate. Semisynthetic ferruginol (1) and some selected analogues, together with the synthesized analogues, were tested in vitro for the inhibition of proliferation in four breast cancer cell lines, SUM149, MDA-MB231, T47D, and MCF07. As a result, several tested abietane analogues decreased cell proliferation and enhanced cell death, with IC50 in the range 1.3-18.7 ¿M. This work demonstrates the antitumor activities of two tested compounds, making these molecules interesting for the development of new anticancer agents. |
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