Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


MDR Reversal by Deprenylated Tetracyclic and Hexacyclic Analogues of N-Acetylardeemin: Confirmation of the Ardeemin Pharmacophore

Author(s): Carmen Avendano, Esmeralda Caballero, Cristina Mendez-Vidal, Ana R. de Quesada, J. Carlos Menendez.


The MDR chemosensitising activity of several analogues of the ardeemins, including five derivatives of the ABCD fragment, nine derivatives of the complete hexacyclic framework and one seco analogue lacking the B ring was studied. The results obtained confirm that the pharmacophoric moiety of the ardeemins as MDR reversers is located at their DEF fragment, and suggest that the epimer of the ardeemins at the alanine stereocenter should be more active than the natural stereoisomer.

Keywords: Antitumour drug resistance, MDR, glycoprotein P-170, ardeemin, pharmacophore

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Article Details

Year: 2006
Page: [369 - 377]
Pages: 9
DOI: 10.2174/157018006777805558
Price: $58