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  • Title: Chiral salicyl diamines: potent anticancer molecules.
    Author: Gao J, Liu YG, Zhou Y, Zingaro RA.
    Journal: ChemMedChem; 2007 Dec; 2(12):1723-9. PubMed ID: 17943711.
    Abstract:
    A set of 12 enantiomeric diamine-based small molecules was synthesized and screened for anticancer activity against five human cancer cell lines: NCI-H460, A549, MCF-7, SK-BR-3, and T-47D. The salicyl diamino compounds (1-6) were found to induce inhibition of the growth of cancer cells at submicromolar concentrations. The lead compound, N,N'-bis-salicyl-(1R,2R)-diaminocyclohexane (1) displayed single-reagent anticancer activity with an IC(50) value equal to or less than 2.0 microM in H460 and A-549 cancer cells. SRB and colony formation assays indicated that compound 1 shows greater cytotoxic activity toward MCF-7 cells than MCF-10A cells. Real-time RT-PCR analysis demonstrated that compound 1, is an extremely efficient regulator of antiapoptotic genes, Bcl-xL, Bcl-2, and the cell cycle related gene, cyclin D1. This study provides a new insight into the development of novel small molecules in the treatment of human breast cancers.
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