Title: Cytotoxic 4'-aminochalcones and related compounds
Authors: Dimmock, J R ×
Jha, A
Zello, G A
Allen, T M
Santos, C L
Balzarini, Jan
De Clercq, Erik
Manavathu, E K
Stables, J P #
Issue Date: Apr-2003
Series Title: Die Pharmazie vol:58 issue:4 pages:227-232
Abstract: A series of 4'-aminochalcones 1 and related maleamic acids 2 and Schiff bases 3 were designed and synthesized as candidate cytotoxic agents. The atomic charges on different atoms of representative compounds were calculated. Evaluation of the enones 1-3 against human Molt 4/C8 and CEM T-lymphocytes as well as murine P388 and L1210 leukemic cells revealed that approximately 40% of the IC50 values generated were less than 10 microM. In some cases cytotoxicity was correlated with the Hammett sigma values of the aryl substituents and less frequently with the aryl Hansch pi values. Evidence was obtained that in general these compounds displayed selective toxicity for certain malignant cells and were well tolerated in mice. This study has revealed various directions whereby the project may be amplified in the future with a view to finding compounds with increased cytotoxicity to tumour cells.
ISSN: 0031-7144
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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