A new series of 3-benzoylamino-5-(1H-imidazol-4-yl)methylaminobenzo[b]furans were synthesized and screened as antitumor agents. As a general trend, tested compounds showed concentration-dependent antiproliferative activity against HeLa and MCF-7 cancer cell lines, exhibiting GI50values in the low micromolar range. In most cases, insertion of a methyl substituent on the imidazole moiety improved the antiproliferative activity. Therefore, methyl-imidazolyl-benzo[b]furans compounds were tested in cell cycle perturbation experiments, producing cell cycle arrest with proapoptotic effects. Their core similarity to known colchicine binding site binders led us to further study the structure features as antitubulin agents by in silico protocols.
|Number of pages||11|
|Journal||CHEMICAL BIOLOGY & DRUG DESIGN|
|Publication status||Published - 2018|
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
- Organic Chemistry
Buscemi, S., Gentile, C., Lauria, A., Delisi, R., Bartolotta, R., Palumbo Piccionello, A., Martorana, A., Delisi, R., & Mingoia, F. (2018). Design, synthesis, and biological evaluation of a new class of benzo[b]furan derivatives as antiproliferative agents, with in silico predicted antitubulin activity. CHEMICAL BIOLOGY & DRUG DESIGN, 91, 39-49.