Synthesis of monomeric and dimeric steroids containing [1,2,4]triazolo[1,5-a]pyrimidines
2016; Elsevier BV; Volume: 116; Linguagem: Inglês
10.1016/j.steroids.2016.09.014
ISSN1878-5867
AutoresAiled Arenas-González, Luis Antonio Mendez-Delgado, Penélope Merino‐Montiel, José M. Padrón, Sara Montiel‐Smith, José Luis Vega-Báez, Socorro Meza‐Reyes,
Tópico(s)Synthesis and Biological Evaluation
ResumoThe synthesis of several monomeric and dimeric steroidal [1,2,4]triazolo[1,5-a]pyrimidines (TPs) derived from steroids are described. These derivatives were prepared from α,β-unsaturated carbonyl compounds through a Claisen Schmidt condensation and rearrangement of the spiro moiety followed by a cycloaddition with 3-amino-1,2,4-triazole. The antiproliferative activity of compounds 7, 13–15 was tested against human cancer cells; several IG50 values were below 10 μM.
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