Synthesis and biological evaluation of novel steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines

The preparation of steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines and their biological evaluation as potential anticancer agents are herein reported. These novel heterosteroids (2, 4) were prepared through the condensation reaction of 3-amino-1,2,4-triazole with 16-arylidene-17-ketosteroids (1, 3). All the synthesized compounds were evaluated for their anticancer activity in vitro against PC-3 (human prostatic carcinoma), MCF-7 (human breast carcinoma) and EC9706 (human esophageal carcinoma) cell lines. Among the screened compounds, 2i, 2n and 4f showed significant inhibitory activity against all the three human cell lines.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A novel class of steroidal[17,16-d]triazolopyrimidines was synthesized. ► These heterosteroids contain the 1,2,4-triazolo[1,5-a]pyrimidine moiety. ► Some of the synthesized compounds showed promising anticancer activity.