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

Abstract EN

Derivatives (1-15) of steroidal and indole class were synthesized using different strate gies.

These compounds were characterized by 'H 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 treat ment 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 (IC so = 21.35 µg/mL) and 1 (ICso = 22.50 µg/mL) showed highest inhibitory activities as com pared to compounds 2 (IC s0= 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.