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Using androstenedione as the starting material, we have synthesised 11 novel 4-chloro-16-(E)-benzylidene androst-1,4-diene-3,17-dione derivatives. All the final products are novel and were identified by ¹H NMR, 13C NMR and HRMS spectrometry. [ABSTRACT FROM AUTHOR]

The synthesis of steroidal derivatives containing [1,2,4]triazolo[1,5-a]pyrimidine derived from progesterone is described. The Claisen condensations of Δ1,4-pregnadien-3,20-dione and 4-chloro-Δ1,4-pregnadien-3,20-dione with dimethyl oxalate afforded 21-methoxalylpregn-1,4-diene-3,20-dione and 4-chloro-21-methoxalylpregn-1,4-diene-3,20-dione, respectively. Furthermore, the reactions of these compounds with 3-amino-1,2,4-triazole yielded the corresponding [1,2,4]triazolo[1,5-a]pyrimidine derivatives. The newly synthesised compounds were evaluated in vitro by means of sulforhodamine B assays for antiproliferative activity against HeLa and MCF-7 cells. [ABSTRACT FROM AUTHOR]