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期刊论文
Synthesis and anticancer activity of 2-alkylaminomethyl-5-diaryl-methylenecyclopentanone hydrochlorides and related compounds
Bioorganic & Medicinal Chemistry 2005(13)1285-1291,-0001,():
Eleven new diaryl-methylenecyclopentanone Mannich hydrochlorides and related compounds were synthesized with different modification on Mannich base and α, β-unsaturated bonds. The glutathione-binding ability, glutathione-S-transferase π(GSTπ) inhibition and antitumor effect of these compounds were compared. Compounds containing both Mannich base and α-unsaturated bond have GSH binding ability, GSTπ inhibitory activity and antitumor effect. Compounds without Mannich base or having a α-saturated bond lose GSH binding ability and the antitumor effect. Converting of Mannich base from dimethylaminomethyl group to morpholino, pyrrolidino, or piperidino-methyl groups do not evidently change the antitumor effect. However replacement of phenyl group with methylphenyl group on β-chain significantly increases cytotoxic effect in breast cancer cells but not in immortalized mammary epithelial cells. Our data suggest that diaryl-methylenecyclopentanones represent a new category of compounds which might inhibit tumor growth through binding to glutathione or thiol proteins.
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