| Popis: |
One pot Click chemistry is employed to link trizole and benzimidazole pharmacophore to get N-((1-((1H-benzo[d]imidazol-2-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)aniline and its derivatives. Flexible linkages in the form of –CH2-R or –O-R/ -N-R were designed during synthesis. All the newly synthesized compounds were characterized by FT-IR and NMR spectroscopy as well as high resolution mass spectrometry. 1H NMR study showed interesting fluxional rotation in one of the molecules due to intramolecular hydrogen bonding. Selected compounds were screened for in vitro anti-proliferative activity using NCI (National Cancer Institute)-60-human-tumor-cell line-screening program. The most potent structure N-((1-((1H-benzo[d]imidazol-2-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)-4-chloroaniline7e showed 40% growth inhibition in renal cancer cell line (UO-31) at 10 µM concentration. |
