Design, Synthesis and Antitumor Activity Evaluation of Indole Derivatives Containing Thiadiazole and Urea Motifs

Abstract A series of novel indole derivatives incorporating urea structural fragments and 1,3,4‐thiadiazole moieties ( E1‐25 ) were designed and synthesized. The antiproliferative activity of these compounds was assessed using methyl thiazolyl tetrazolium (MTT) assay in four human cancer cell lines, human lung adenocarcinoma cells A549 (A549), prostate cancer cells PC‐3 (PC‐3), human chronic myeloid leukemia cells (K562), human urinary bladder carcinoma cell line (5637). The results revealed that several compounds exhibited antiproliferative activity, with compound E25 showing promising activity against K562 cells, with an IC 50 value of 9.42 µM. The mechanism of action of compound E25 was further investigated using apoptosis analysis, which provided evidence of its significant ability to induce cell apoptosis.