Title: Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds
Authors: Dimmock, Jonathan R ×
Jha, Amitabh
Kumar, Praveen
Zello, Gordon A
Quail, J Wilson
Oloo, Eliud O
Oucharek, Jennifer J
Pasha, Mohammed K
Seitz, Dallas
Sharma, Rajendra K
Allen, Theresa M
Santos, Cheryl L
Manavathu, Elias K
De Clercq, Erik
Balzarini, Jan
Stables, James P #
Issue Date: Jan-2002
Series Title: European journal of medicinal chemistry vol:37 issue:1 pages:35-44
Abstract: A series of 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes 2a-c and 4 and a related acyclic analogue 6a were synthesised and converted to the corresponding Mannich bases 3a-c, 5 and 6b. Evaluation of these compounds against murine P388 and L1210 cells as well as human Molt 4/C8 and CEM T-lymphocytes revealed that the Mannich bases were more cytotoxic than the corresponding unsaturated ketones. 1,4-bis(3-Dimethylaminomethyl-2-oxo-1-cyclohexylmethylene)benzene dihydrochloride (3a) had lower IC(50) values than melphalan against the four cell lines and was 15 times more potent than this drug when examined against a panel of human tumours.
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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