Title: 1-Aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides and related adducts: A quest for selective cytotoxicity for malignant cells
Authors: Pati, Hari N ×
Das, Umashankar
Kawase, Masami
Sakagami, Hiroshi
Balzarini, Jan
De Clercq, Erik
Dimmock, Jonathan R #
Issue Date: May-2008
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:16 issue:10 pages:5747-5753
Abstract: The primary objective of this study was to discover one or more clusters of compounds which are not equitoxic but display cytoselectivity toward different malignant cells. Furthermore a most important consideration is that such molecules should also display greater cytotoxic potencies to tumors than normal tissues. Two series of compounds are described which meet these criteria, namely the 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides 1a-e and 1-aryl-3-dimethylamino-2-hydroxymethyl-1-propanone hydrochlorides 2a-e. A number of these compounds possess marked cytotoxic potencies (IC(50) and CC(50) values within the 10(-6) and 10(-7) molar range) which are greater than these of the reference drug melphalan. Statistical analyses demonstrated that cytotoxic potencies are influenced by the size of the aryl substituents in series 1 and to some extent by the electronic properties of the aryl groups in series 2. The mode of action of a representative compound 1e in HL-60 cells included inducing apoptosis and activation of caspases -3, -8, and -9.
ISSN: 0968-0896
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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