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Title: The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones
Authors: Pati, Hari N ×
Das, Umashankar
Das, Swagatika
Bandy, Brian
De Clercq, Erik
Balzarini, Jan
Kawase, Masami
Sakagami, Hiroshi
Stables, James P
Quail, J Wilson
Dimmock, Jonathan R #
Issue Date: Jan-2009
Series Title: European Journal of Medicinal Chemistry vol:44 issue:1 pages:54-62
Abstract: This study demonstrated that replacement of the axial protons on the C2 and C6 atoms of various 1-methyl-3,5-bis(benzylidene)-4-piperidones 3 by a dimethylene bridge leading to series 2 lowered cytotoxic potencies. Four compounds 2a and 3a-c emerged as lead molecules based on their toxicity towards different neoplasms and their selective toxicity for malignant rather than normal cells. Some possible reasons for the disparity between the IC(50) values in the two series of compounds are presented based on molecular modeling, logP values and respiration in rat liver mitochondria.
URI: 
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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