Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 43, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128097
Keywords
Benzimidazole-pyrazole; Antiproliferative activity; Cells apoptosis; Cell cycle
Categories
Funding
- Science and Technology Department of Shaanxi Province [2020NY153]
- National Natural Science Foundation of China [21542016]
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Novel pyrazole-benzimidazole derivatives were designed, synthesized, and evaluated for their antiproliferative activity against cancer cell lines, showing compounds with significant potential for inducing apoptosis and cell cycle arrest in cancer cells.
A series of novel pyrazole-benzimidazole derivatives (6-42) have been designed, synthesized and evaluated for their in vitro antiproliferative activity against the HCT116, MCF-7 and Huh-7 cell lines. Among them, compounds 17, 26 and 35 showed significant antiproliferative activity against HCT116 cell lines with the IC50 values of 4.33, 5.15 and 4.84 mu M, respectively. Moreover, fluorescent staining studies showed compound 17 could induce cancer cells apoptosis. The flow cytometry assay revealed that compound 17 could induce cell cycle arrest at G0/G1 phase. All in all, these consequences suggest that pyrazole-benzimidazole derivatives could serve as promising compounds for further research to develop novel and highly potent cancer therapy agents.
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