@article{aa3f6dc93e25439798cbbcfe383a40c7,
title = "Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds",
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 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.",
keywords = "Cytotoxicity, Mannich bases, N-myristoyltransferase, X-ray crystallography, α,β-unsaturated ketones",
author = "Dimmock, {Jonathan R.} and Amitabh Jha and Praveen Kumar and Zello, {Gordon A.} and Quail, {J. Wilson} and Oloo, {Eliud O.} and Oucharek, {Jennifer J.} and Pasha, {Mohammed K.} and Dallas Seitz and Sharma, {Rajendra K.} and Allen, {Theresa M.} and Santos, {Cheryl L.} and Manavathu, {Elias K.} and {De Clercq}, Erik and Jan Balzarini and Stables, {James P.}",
note = "Funding Information: The authors thank the following organisations for financial support for the study, namely Purdue Neuroscience Company, USA (J.R.D., A.J., P.K.), Natural Sciences and Engineering Research Council of Canada (J.W.Q.), University of Saskatchewan (E.O.O.), Canadian Institutes of Health Research (R.K.S.), National Cancer Institute of Canada (T.M.A.), Belgian Fonds voor Geneeskundig Wetenschappelijk Onderzoek (E.D.C., J.B.) and the National Institute of Neurological Disorders and Stroke, USA (J.P.S.). In addition, the National Cancer Institute, USA, kindly undertook the bioevaluations using a panel of human tumour cell lines. ",
year = "2002",
month = jan,
day = "1",
doi = "10.1016/S0223-5234(01)01294-6",
language = "English (US)",
volume = "37",
pages = "35--44",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson SAS",
number = "1",
}