Synthesis and anticancer activity of glycol-bridged bis-benzimidazoles\n
A series of bis-benzimidazoles with polyglycol-sulfide linker were prepared and tested for their tumor cell growth inhibitory activities. Two derivatives (2c and 3a) showed significant growth inhibitory activities against 518A2 melanoma cells. In addition, these compounds were active against multidrug resistant KB-V1Vbl cervix carcinoma cells (vinblastine-resistant cells with overexpressed P-gp transporter) and MCF-7Topo breast carcinoma cells (topotecan-resistant cells with overexpressed BCRP transporter). Thus, we have identified valuable lead structures for the design of new anticancer drugs based on benzimidazole systems that can overcome drug resistance.
Anticancer drugs, Benzimidazole, Glycol, Multidrug resistance, Thioether.