| Literature DB >> 25863023 |
Tamara G M Treptow1, Fabrício Figueiró2, Elisa H F Jandrey2, Ana M O Battastini2, Christianne G Salbego2, Juliana B Hoppe2, Priscila S Taborda1, Sabrina B Rosa1, Luciana A Piovesan1, Caroline Da R Montes D'Oca3, Dennis Russowsky3, Marcelo G Montes D'Oca4.
Abstract
We described the first synthesis of fatty acid 3,4-dihydropyrimidinones (DHPM-fatty acids) using the Biginelli multicomponent reaction. Antiproliferative activity on two glioma cell lines (C6 rat and U-138-MG human) was also reported. The novel DHPM-fatty acids reduced glioma cell viability relative to temozolomide. Hybrid oxo-monastrol-palmitic acid was the most potent, reducing U-138-MG human cell viability by ca. 50% at 10 μM. In addition, the DHPM-fatty acids showed a large safety range to neural cells, represented by the organotypic hippocampal culture. These results suggest that the increased lipophilicity of DHPM-fatty acids offer a promising approach to overcoming resistance to chemotherapy and may play an important role in the development of new antitumor drugs.Entities:
Keywords: Antiproliferative activity; Fatty acids; Glioma cell; Monastrol; Oil chemistry
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Year: 2015 PMID： 25863023 DOI： 10.1016/j.ejmech.2015.03.062
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514