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Novel hybrid DHPM-fatty acids: Synthesis and activity against glioma cell growth in vitro

2015; Elsevier BV; Volume: 95; Linguagem: Inglês

10.1016/j.ejmech.2015.03.062

1768-3254

Tamara G.M. Treptow, Fabrício Figueiró, Elisa Helena Farias Jandrey, Ana Maria Oliveira Battastini, Christianne Gazzana Salbego, Juliana Bender Hoppe, Priscila S. Taborda, Sabrina B. Rosa, Luciana A. Piovesan, Caroline Da Ros Montes D’Oca, Dennis Russowsky, Marcelo G. Montes D’Oca,

Synthesis of heterocyclic compounds

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.