461676-11-9Relevant academic research and scientific papers
Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds
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
, p. 35 - 44 (2002)
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 IC50 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.
