Abstract
α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone 5 showed superior antitumor activity in vivo with both oral and intraperitoneal administration at 3 mg/kg. Cell-based mechanism of action studies demonstrated that 5 induced cell accumulation at sub-G1 and G2/M phases without interfering with microtubule polymerization. Furthermore, several cancer cell growth-related proteins were identified by using chalcone 5 as a bait for the affinity purification of binding proteins.
Highlights
A small change in a chemical structure sometimes induces a big change in a biological profile
In our continuing structure–activity relationship (SAR) study of chalcone derivatives as anti-prostate cancer agents [4,5], we explored whether the insertion of fluorine and/or a fluorinated functional group into synthetic chalcones would improve their activity
The values are average ± SD of three independent experiment. b Antiproliferative activity expressed as IC50 values for each cell line, the concentration of compound that caused 50% reduction relative to untreated cells determined by the SRB assay
Summary
A small change in a chemical structure sometimes induces a big change in a biological profile. The chalcones containing electron withdrawing group on ring-B (2, 4, and 5) showed more potent antiproliferative activity than the remaining compounds (Table 2). B Antiproliferative activity expressed as IC50 values for each cell line, the concentration of compound that caused 50% reduction relative to untreated cells determined by the SRB assay. Chalcone 5 showed significant antiproliferative activity against these cells with IC50 values of 0.14–0.28 μM (Table 3). Chalcone 5 showed significant antiproliferative activity against these cells with IC50 va4luofe1s3 of 0.14–0.28 μM (Table 3). Five main bands were detected by staining with Coumassie Brilliant Blue (CBB) dye, corresponding to proteins with molecrole in the maintenance of mitochondrial crista structure [29] and PA2G4 isoforms display opposing functions, i.e., suppressive and promoting effects, in cancer [30]. The purity of all compounds was determined as >95% by 1H NMR
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