Synthesis and in vitro anti-proliferative capabilities of steroidal thiazole and indole derivatives

Derivatives (1–15) of steroidal and indole class were synthesized using different strategies. These compounds were characterized by ¹H NMR spectroscopy and EI-MS, respectively. The synthetic derivatives were examined for their cytotoxic effects on human adenocarcinoma cells (HCT-116) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and morphometric analysis. The cytotoxic effects of all the compounds were observed after 48 h treatment and it was found that out of fifteen, four compounds 1, 2, 3, and 14 showed inhibitory action on the cancer cells. We have calculated the IC₅₀ values for compounds 1, 2, 3, and 14 which were 22.50 µg/mL, 55.65 µg/mL, 21.35 µg/mL and 58.50 µg/mL, respectively. The compounds 3 (IC₅₀ = 21.35 µg/mL) and 1 (IC₅₀ = 22.50 µg/mL) showed highest inhibitory activities as compared to compounds 2 (IC₅₀ = 55.65 µg/mL) and 14 (IC₅₀ = 58.50 µg/mL). These results suggested that steroidal thiazole and indole derivatives are potent lead molecules having strong anti-cancer proliferative capabilities.