Synthesis of some novel 4-benzothiazol-2-yl-benzoyl-1H-pyrazoles, and evaluation as antiangiogenic agents

摘要

Some 4-(1,3-benzothiazol-2-yl)-benzoyl-1H-pyrazole derivatives have been synthesized by reaction of o-aminothiophenol (1) with different electrophilic and nucleophilic reagents. All of the newly synthesized compounds were evaluated for cytotoxicity against breast cancer cell line MCF-7. Two of the compounds were more potent than tamoxifen and three were as potent as tamoxifen. These results were consistent with percentage inhibition of human VEGF compared with control untreated cells.