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1
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0026051430
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Sears M.R., Burrows B., Flannery E.M., Herbison G.P., Hewitt C.J., and Holdaway M.D. N. Eng. J. Med. 325 (1991) 1067
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Sears, M.R.1
Burrows, B.2
Flannery, E.M.3
Herbison, G.P.4
Hewitt, C.J.5
Holdaway, M.D.6
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2
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0024491638
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Burrows B., Martinez F.D., Halonen M., Barbee R.A., and Cline M.G. N. Eng. J. Med. 320 (1989) 271
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Burrows, B.1
Martinez, F.D.2
Halonen, M.3
Barbee, R.A.4
Cline, M.G.5
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5
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0027729893
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Dombrowicz D., Flamand V., Brigmann K.K., Koller B.H., and Kinet J.P. Cell 75 (1993) 969
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(1993)
Cell
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Dombrowicz, D.1
Flamand, V.2
Brigmann, K.K.3
Koller, B.H.4
Kinet, J.P.5
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7
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0035974653
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Representative examples include:
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Representative examples include:. Berger M., Albrecht B., Berces A., Ettmayer P., Neruda W., and Woisetschlaeger M. J. Med. Chem. 44 (2001) 3031
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J. Med. Chem.
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Berger, M.1
Albrecht, B.2
Berces, A.3
Ettmayer, P.4
Neruda, W.5
Woisetschlaeger, M.6
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8
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0031055629
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Hasegawa M., Takenouchi K., Takahashi K., Takeuchi T., Komoriya K., Uejima Y., and Kamimura T. J. Med. Chem. 40 (1997) 395
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Hasegawa, M.1
Takenouchi, K.2
Takahashi, K.3
Takeuchi, T.4
Komoriya, K.5
Uejima, Y.6
Kamimura, T.7
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9
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33746220690
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note
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50 values were calculated and data normalized to an internal standard to take into account donor to donor variability. The cytotoxicity of compounds was also evaluated and shown to be unrelated to efficacy. For selected compounds, compound concentration was evaluated during the course of the experiment and was shown to remain unchanged.
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10
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33746264228
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note
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Compounds (1 μM) were incubated at 37 °C with human liver microsomes (0.5 μM) for 60 min. Concentration of compound was measured over the time course of the experiment and used to determine a disappearance half-life.
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11
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33746264227
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Compounds (1 μM) were incubated at 37 °C with recombinant CYP1A1 or CYP1A2 (0.15 μM) for 60 min. Concentration of compound was measured over the time course of the experiment and used to determine a disappearance half-life.
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12
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0032414615
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CYP1A1 is predominantly expressed in extra-hepatic tissues. See:
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CYP1A1 is predominantly expressed in extra-hepatic tissues. See:. Smith G., Stubbins M.J., Harries L.W., and Wolf C.R. Xenobiotica 28 (1998) 1129
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(1998)
Xenobiotica
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, pp. 1129
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Smith, G.1
Stubbins, M.J.2
Harries, L.W.3
Wolf, C.R.4
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15
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0141538249
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For CYP1A enzymes see, for example:
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For CYP1A enzymes see, for example:. Lewis D.F.V. Current Med. Chem. 10 (2003) 1955
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(2003)
Current Med. Chem.
, vol.10
, pp. 1955
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Lewis, D.F.V.1
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17
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33746260679
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note
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It is likely that the reduced lipophilicity of these compounds also contributes to their increased metabolic stability.
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18
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33746220642
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note
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2O requires C, 52.15; H, 6.71; N, 22.81%.
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19
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0026768492
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Bonnet P.A., Michel A., Laurent F., Sablayrolles C., Rechencq E., Mani J.C., Boucard M., and Chapat J.P. J. Med. Chem. 35 (1992) 3353
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(1992)
J. Med. Chem.
, vol.35
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Bonnet, P.A.1
Michel, A.2
Laurent, F.3
Sablayrolles, C.4
Rechencq, E.5
Mani, J.C.6
Boucard, M.7
Chapat, J.P.8
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21
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33746220643
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note
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Despite extensive experimentation we were unable to ascertain the specific mechanism of action for these compounds.
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