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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells.

Fifteen 4-phenyl-3,5-dibenzoyl-1,4-dihydropyridines (BzDHPs) (1-15) substituted at the 4-phenyl ring were synthesized and compared to their cytotoxic activity and multidrug resistance (MDR)-reversing activity in in vitro assay systems. Among them, 2-CF3 (5) (IC50=8.7 microM), 2-Cl (11) (IC50=7.0 microM) and 3-Cl (12) (IC50=7.0 microM) derivatives showed the highest cytotoxic activity against human oral squamous carcinoma (HSC-2) cells. The activity of P-glycoprotein ( Pgp) response for MDR in tumor cells was reduced by some of derivatives (3, 4, 8, 12), verapamil (VP) and nifedipine (NP). These data suggest that 3,5-dibenzoyl-4-(3-chlorophenyl)-1,4-dihydro-2,6-dimethylpyridine (12) can be recommended as a new drug candidate for MDR cancer treatment.[1]

References

  1. 3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Kawase, M., Shah, A., Gaveriya, H., Motohashi, N., Sakagami, H., Varga, A., Molnár, J. Bioorg. Med. Chem. (2002) [Pubmed]
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