Studies on 6,11-Bisthiatetracyclic- and pentacyclic Steroidal Analogues: Syntheses, Characterization, Antimicrobial-, Antituberculosis-, Antitumor- and DNA Cleavage Activity of New Pyrazole-, Isoxazole-, Pyrimidine-, and Benzodiazepine Frameworks

Abstract

A series of new heterocyclic steroidal analogues has been synthesized from the reactions of the key intermediates 5 and 6. All these compounds were evaluated for bioactivity. In the benzodiazepine series 17-20, the 1,2-Diphenylethane-1,2-diamine substituted compounds 19 and 20 displayed the highest activity with IC₅₀ equal to 13 and 12 µM for HeLa cell, and 12 and 10 µM for HCT116 cell. Similarly these compounds (19 and 20) showed higher activity than chloroamphenicol against Klebsiella pneumoniae and Escherichia coli and behaved as the most promising being active against M. tuberculosis (H37Rv) with MIC 7.7 and 7.3 µM respectively. Moreover, the compounds were subjected for DNA cleavage potential by gel electrophoresis method.