Synthesis and in vitro antiproliferative activity of new 1,3,4-oxadiazole derivatives possessing sulfonamide moiety

• Synthesis and in vitro antiproliferative activities of new oxadiazoles are reported.
• Compound 1k demonstrated the highest mean %inhibition over NCI-58 cell line panel.
• Compound 1k exerted high and broad-spectrum antiproliferative activity.
• Compound 1k inhibited the growth of T-47D and MDA-MB-468 breast cancer cell lines by 90.47% and 84.83%, respectively.
• Compound 1k showed superior activity than Paclitaxel and Gefitinib against the most sensitive cell lines.

Synthesis of a new series of 1,3,4-oxadiazole derivatives possessing sulfonamide moiety is described. Their in vitro antiproliferative activities against NCI-58 human cancer cell lines of nine different cancer types were tested. Compound 1k with p-methoxybenzenesulfonamido moiety showed the highest mean %inhibition value over the 58 cell line panel at 10 μM concentration. It showed broad-spectrum antiproliferative activity over many cell lines of different cancer types. For instance, compound 1k inhibited the growth of T-47D breast cancer cell line by 90.47% at 10 μM. And it inhibited growth of SR leukemia, SK-MEL-5 melanoma, and MDA-MB-468 breast cancer cell lines by more than 80% at the same test concentration. Compound 1k showed superior activity than Paclitaxel and Gefitinib against the most sensitive cell lines.

A series of new 1,3,4-oxadiazole derivatives possessing sulfonamide moiety was synthesized. Their in vitro antiproliferative activities against NCI-58 cancer cell line panel are reported.Figure optionsDownload as PowerPoint slide