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Title: Cytotoxic 1,3-diarylidene-2-tetralones and related compounds
Authors: Dimmock, Jonathan R ×
Padmanilyam, Maniyan P
Zello, Gordon A
Quail, J Wilson
Oloo, Eliud O
Prisciak, Jared S
Kraatz, Heinz Bernhard
Cherkasov, Arten
Lee, Jeremy S
Allen, Theresa M
Santos, Cheryl L
Manavathu, Elias K
De Clercq, Erik
Balzarini, Jan
Stables, James P #
Issue Date: Oct-2002
Series Title: European journal of medicinal chemistry vol:37 issue:10 pages:813-24
Abstract: A number of 1,3-arylidene-2-tetralones 1, 2 and 4 were synthesised and demonstrated cytotoxic activity towards murine P388 and L1210 cells as well as human Molt 4/C8 and CEM T-lymphocytes. In general, the related 1-arylidene-2-tetralones 3 possessed lower potencies in these screens than the compounds in series 1 and 4. Approximately, half of the compounds were evaluated against a panel of human tumour cell lines. In this screen, most of the enones were more cytotoxic than the established anticancer agent melphalan and some demonstrated selective toxicity towards leukemic and colon cancer cells. The modes of action of representative compounds include interfering with the biosyntheses of nucleic acids and proteins as well as altering redox potentials. The compounds were well tolerated when administered intraperiteonally to mice. Thus these novel enones are promising prototypic molecules due to their potent cytotoxic properties and lack of significant murine toxicity.
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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