Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines

Novel 1,4-benzodiazepine compounds were synthesized and evaluated for their ability to inhibit the proliferation of tumor cells. Some compounds revealed activities in the micromolar range and were more efficient than reference compound Ro 5-4864. Preliminary SAR helped to identify critical motifs for antiproliferative activity and led to the discovery of a compound selective for a melanoma cell line, known for its resistance to chemotherapy.

Graphical abstractNovel 1,4-benzodiazepine compounds were synthesized and displayed antiproliferative activities in the micromolar range against tumor cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide