Synthesis of monomeric and dimeric steroids containing [1,2,4]triazolo[1,5-a]pyrimidines
Ailed Arenas-González1, Luis Antonio Mendez-Delgado1, Penélope Merino-Montiel1
1Benemérita Universidad Autónoma de Puebla, Facultad de Ciencias Químicas, Ciudad Universitaria, C.P. 72570 Puebla, Pue., Mexico.
Abstract:
The 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 10μM.
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