DESIGN AND SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS

摘要

A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC₅₀ of 2.1 muM.