Structure−Activity Relationship Studies on Benzofuran Analogs of
Propafenone-Type Modulators of Tumor Cell Multidrug Resistance
Posted on 1996-11-22 - 00:00
A series of benzofurylethanolamine analogs of
propafenone (1a) have been prepared and
evaluated for multidrug resistance-reversing activity in two in vitro
assay systems. As for
propafenones, an excellent correlation of biological data with
calculated lipophilicity values
was found for benzofurans, whereby the latter generally had lower
activity/lipophilicity ratios.
Almost identical slopes of the regression lines were obtained for
both propafenones and
benzofurans. Multiple linear regression analysis of the complete
data set yielded an equation
with excellent predictive power
(r2cross-valid = 0.968).
Interaction measurements with artificial
membranes indicated that the differences in activity between these two
series of compounds
are not due to differences in the interaction pattern with biological
membranes.
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Ecker, Gerhard; Chiba, Peter; Hitzler, Manuela; Schmid, Diethard; Visser, Klaus; Cordes, Hans Peter; et al. (2016). Structure−Activity Relationship Studies on Benzofuran Analogs of
Propafenone-Type Modulators of Tumor Cell Multidrug Resistance. ACS Publications. Collection. https://doi.org/10.1021/jm960384x
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AUTHORS (9)
GE
Gerhard Ecker
PC
Peter Chiba
MH
Manuela Hitzler
DS
Diethard Schmid
KV
Klaus Visser
HC
Hans Peter Cordes
JC
Josef Csöllei
JS
Joachim K. Seydel
KS
Klaus-Jürgen Schaper