Biological Evaluation of Hetero-Cyclic Steroidal Analogues. Syntheses, Characterization, and Biological Evaluation

      Аннотация: Heterocyclic compounds containing nitrogen, oxygen or sulfur are by far the most common. Compounds containing nitrogen/sulfur, in general, possess potent bioactivity. Thiochroman-4-one and 3,4-dihydrobenzo[b]thiepin-5(2H)-one are versatile reagents that have been extensively utilized in heterocyclic synthesis. A series of pyrazole carboxamides were synthesized and evaluated for antibacterial and antifungal activity. All compounds were screened for their cytotoxic activity against two tumor cell lines, namely the human colon tumor cell line (HCT116) and the human cervical cancer cell line (HeLa). Most of the tested compounds exhibited potent antitumor activity and antituberculosis activity. Novel pyrazole-, oxazole-, pyrimidine- and benzodiazepine derivatives containing thiochromeno- and benzothiepino moieties were prepared via the reaction of the diketo ester with appropriate chemical reagents. Single-crystal XRD studies have been done on some of the compounds. Benzodiazepine derivatives displayed the highest activity among the tested compounds with HeLa cell and HCT116 cell and more active against H37Rv, compared to other analogs.

Ключевые слова: Heterocyclic steroidal analogoues, Thiochromonone, Benzthepinone, Antibacterial activity, anticancer activity, Anti-tuberculosis Activity