Eliud O. Oloo
University of Saskatchewan
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European Journal of Medicinal Chemistry | 2000
Jonathan R. Dimmock; Praveen Kumar; Adil J. Nazarali; Narasimhan L. Motaganahalli; Travis P. Kowalchuk; Michael A Beazely; J. Wilson Quail; Eliud O. Oloo; Theresa M. Allen; Jennifer Szydlowski; Erik Desire Alice Declercq; Jan Balzarini
A number of 2-arylidenecyclohexanones 1, 2, 6-bis(arylidene)cyclohexanones 2 and related Mannich bases 3-5 were prepared. Various torsion angles as well as atomic charges on olefinic carbon atoms were determined by molecular modelling on all compounds. These molecules showed cytotoxicity towards murine P388 and L1210 cells as well as to human Molt 4/C8 and CEM T-lymphocytes. The average cytotoxicity of the dienones 2 was more than three times greater than was found with the monoarylidene analogues 1, and, in general, were slightly more cytotoxic than the Mannich bases 3-5. A number of the compounds displayed potency towards a panel of human tumour cell lines and most of the representative compounds in series 2-5 were selectively toxic to colon cancers and leukaemic cells.
European Journal of Medicinal Chemistry | 2002
Jonathan R. Dimmock; Amitabh Jha; Gordon A. Zello; J. Wilson Quail; Eliud O. Oloo; Kurt H. Nienaber; Earl S Kowalczyk; Theresa M. Allen; Cheryl Santos; Erik De Clercq; Jan Balzarini; Elias K. Manavathu; James P. Stables
A series of 4-carboxychalcones 1 were prepared and coupled to 3,5-bis(phenylmethylene)-4-piperidone (2) giving rise to a novel series of N-[4-(3-aryl-3-oxo-1-propenyl)phenylcarbonyl]-3,5-bis(phenylmethylene)-4-piperidones (3). Molecular simplification of the amides 3 led to the formation of the corresponding N-(3-aryl-1-oxo-2-propenyl)-3,5-bis(phenylmethylene)-4-piperidones (4). A cytotoxic evaluation of the compounds in series 1-4 utilized murine P388 and L1210 cells as well as human Molt 4/C8 and CEM T-lymphocytes. In general, the compounds displayed significant toxicity; the IC(50) values of 54% of the enones were less than 10 microM when all four screens were considered and less than 1 microM for all members of series 3 in the P388 assay. Various correlations were established between the potencies of the compounds in series 1, 3 and 4 and the Hammett sigma, Hansch pi and molecular refractivity constants of the aryl substituents. Several torsion angles and interatomic distances of five representative compounds in series 3 and 4 were determined by X-ray crystallography, some of which contributed to the observed bioactivity. The marked cytotoxicity and lack of murine toxicity of most of the compounds described in this study, as well as their selective toxicity towards different tumour cell lines, revealed that development of the enones 2-4 as novel candidate antineoplastic agents should be pursued.
European Journal of Medicinal Chemistry | 2002
Jonathan R. Dimmock; Maniyan P Padmanilyam; Gordon A. Zello; J. Wilson Quail; Eliud O. Oloo; Jared S. Prisciak; Heinz-Bernhard Kraatz; Arten Cherkasov; Jeremy S. Lee; Theresa M. Allen; Cheryl Santos; Elias K. Manavathu; Erik De Clercq; Jan Balzarini; James P. Stables
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.
European Journal of Medicinal Chemistry | 2002
Jonathan R. Dimmock; Amitabh Jha; Praveen Kumar; Gordon A. Zello; J. Wilson Quail; Eliud O. Oloo; Jennifer J Oucharek; Mohammed Khysar Pasha; Dallas P. Seitz; Theresa M. Allen; Cheryl Santos; Elias K. Manavathu; Erik De Clercq; Jan Balzarini; James P. Stables
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.
Acta Crystallographica Section E: Crystallographic Communications | 2002
Eliud O. Oloo; J. Wilson Quail; Maniyan P. Padmanilayam; Jonathan R. Dimmock
The title compound, C18H14O3, crystallizes in space group P21/c as hydrogen-bonded dimers with crystallographic inversion symmetry.
Journal of Medicinal Chemistry | 2001
Jonathan R. Dimmock; Maniyan P. Padmanilayam; Ramanan Narayan Puthucode; Adil J. Nazarali; Narasimhan L. Motaganahalli; Gordon A. Zello; J. Wilson Quail; Eliud O. Oloo; Heinz-Bernhard Kraatz; Jared S. Prisciak; Theresa M. Allen; Cheryl Santos; Jan Balzarini; Erik De Clercq; Elias K. Manavathu
Journal of Medicinal Chemistry | 2002
Jonathan R. Dimmock; Gordon A. Zello; Eliud O. Oloo; J. Wilson Quail; Heinz-Bernhard Kraatz; Pál Perjési; Ferenc Aradi; Krisztina Takács-Novák; Theresa M. Allen; Cheryl Santos; Jan Balzarini; Erik De Clercq; James P. Stables
Acta Crystallographica Section E-structure Reports Online | 2002
Eliud O. Oloo; J. Wilson Quail; Pál Perjési; Jonathan R. Dimmock
Acta Crystallographica Section E-structure Reports Online | 2002
Eliud O. Oloo; J.W. Quail; Maniyan P. Padmanilayam; Jonathan R. Dimmock
Acta Crystallographica Section E: Crystallographic Communications | 2004
Eliud O. Oloo; Kurt H. Nienaber; J. Wilson Quail; Maniyan P. Padmanilayam; Umashankar Das; Jonathan R. Dimmock