Tridentate bipyrazole compounds with a side-arm as a new class of antitumor agents

• DOI: 10.1007/s11164-012-0993-z
• Publication Date: 2013-01-16T06:50:20Z
• Authors: Fouad Malek; Nihed Draoui; Olivier Feron; Smaail Radi
• Keywords: IC50; MCF-7; Cancer cell lines; MTT assay

Eight tridentate bipyrazole derivatives with different side arms have been prepared in one step and with good yields. The products were screened for their cytotoxic activity against three tumor cell lines—human breast cancer cell line MDA-MB231, human prostate cancer cell line PC3, and human colorectal cell line LoVo, by use of colorimetric MTT assay. Structure–activity relationships reflected the effect of substituted drugs. Among this series, two compounds had remarkable in-vitro antiproliferative activity against the LoVo cell line with IC50 values ranging from 2.6 to 2.7 μg ml−1. All the compounds had suitable drug-like characteristics according to Lipinski’s rule.