-
1
-
-
18444374405
-
-
Davies H., Bignell G.R., Cox C., Stephens P., Edkins S., Clegg S., Teague J., Woffendin H., Garnett M.J., Bottomley W., Davis N., Dicks E., Ewing R., Floyd Y., Gray K., Hall S., Hawes R., Hughes J., Kosmidou V., Menzies A., Mould C., Parker A., Stevens C., Watt S., Hooper S., Wilson R., Jayatilake H., Gusterson B.A., Cooper C., Shipley J., Hargrave D., Pritchard-Jones K., Maitland N., Chenevix-Trench G., Riggins G.J., Bigner D.D., Palmieri G., Cossu A., Flanagan A., Nicholson A., Ho J.W.C., Leung S.Y., Yuen S.T., Weber B.L., Seigler H.F., Darrow T.L., Paterson H., Marais R., Marshall C.J., Wooster R., Stratton M.R., and Futreal P.A. Nature 417 (2002) 949
-
(2002)
Nature
, vol.417
, pp. 949
-
-
Davies, H.1
Bignell, G.R.2
Cox, C.3
Stephens, P.4
Edkins, S.5
Clegg, S.6
Teague, J.7
Woffendin, H.8
Garnett, M.J.9
Bottomley, W.10
Davis, N.11
Dicks, E.12
Ewing, R.13
Floyd, Y.14
Gray, K.15
Hall, S.16
Hawes, R.17
Hughes, J.18
Kosmidou, V.19
Menzies, A.20
Mould, C.21
Parker, A.22
Stevens, C.23
Watt, S.24
Hooper, S.25
Wilson, R.26
Jayatilake, H.27
Gusterson, B.A.28
Cooper, C.29
Shipley, J.30
Hargrave, D.31
Pritchard-Jones, K.32
Maitland, N.33
Chenevix-Trench, G.34
Riggins, G.J.35
Bigner, D.D.36
Palmieri, G.37
Cossu, A.38
Flanagan, A.39
Nicholson, A.40
Ho, J.W.C.41
Leung, S.Y.42
Yuen, S.T.43
Weber, B.L.44
Seigler, H.F.45
Darrow, T.L.46
Paterson, H.47
Marais, R.48
Marshall, C.J.49
Wooster, R.50
Stratton, M.R.51
Futreal, P.A.52
more..
-
3
-
-
12144289677
-
-
Wan P.T.C., Garnett M.J., Roe S.M., Lee S., Niculescu-Duvaz D., Good V.M., Jones C.M., Marshall C.J., Springer C.J., Barford D., and Marais R. Cell 116 (2004) 855
-
(2004)
Cell
, vol.116
, pp. 855
-
-
Wan, P.T.C.1
Garnett, M.J.2
Roe, S.M.3
Lee, S.4
Niculescu-Duvaz, D.5
Good, V.M.6
Jones, C.M.7
Marshall, C.J.8
Springer, C.J.9
Barford, D.10
Marais, R.11
-
5
-
-
42949107275
-
-
note
-
For example, human liver microsome stability values for the parent compounds 1 and 2 were 48% and 87% remaining after 15 min, respectively. The values for 1 and 2 in rat liver microsomes were 40% and 11%, respectively. Solubility values for 1 was 87 μM and for 2 was >100 μM at pH 7.4 (phosphate buffer).
-
-
-
-
6
-
-
1642534327
-
-
Khire U.R., Bankston D., Barbosa J., Brittelli D.R., Caringal Y., Carlson R., Dumas J., Gane T., Heald S.L., Hibner B., Johnson J.S., Katz M.E., Kennure N., Kingery-Wood J., Lee W., Liu X.G., Lowinger T.B., McAlexander I., Monahan M.K., Natero R., Renick J., Riedl B., Rong H., Sibley R.N., Smith R.A., and Wolanin D. Bioorg. Med. Chem. Lett. 14 (2004) 783
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 783
-
-
Khire, U.R.1
Bankston, D.2
Barbosa, J.3
Brittelli, D.R.4
Caringal, Y.5
Carlson, R.6
Dumas, J.7
Gane, T.8
Heald, S.L.9
Hibner, B.10
Johnson, J.S.11
Katz, M.E.12
Kennure, N.13
Kingery-Wood, J.14
Lee, W.15
Liu, X.G.16
Lowinger, T.B.17
McAlexander, I.18
Monahan, M.K.19
Natero, R.20
Renick, J.21
Riedl, B.22
Rong, H.23
Sibley, R.N.24
Smith, R.A.25
Wolanin, D.26
more..
-
8
-
-
42949143385
-
-
Maryanoff, B. E.; Kinny, W. A.; Lawson, E. C.; Luci, D. K.; Marchenko, N.; Sviridov, S. International Patent Application Number; WO2007/081995, pg 243 describes preparation of the N-Boc carbamate (29b) in place of the ethyl carbamate analog used to prepare 7 in Scheme 1.
-
Maryanoff, B. E.; Kinny, W. A.; Lawson, E. C.; Luci, D. K.; Marchenko, N.; Sviridov, S. International Patent Application Number; WO2007/081995, pg 243 describes preparation of the N-Boc carbamate (29b) in place of the ethyl carbamate analog used to prepare 7 in Scheme 1.
-
-
-
-
9
-
-
0001160653
-
-
Kornblum N., Powers J.W., Anderson G.J., Jones W.J., Larson H.O., Levand O., and Weaver W.M. J. Am. Chem. Soc. 79 (1957) 6562
-
(1957)
J. Am. Chem. Soc.
, vol.79
, pp. 6562
-
-
Kornblum, N.1
Powers, J.W.2
Anderson, G.J.3
Jones, W.J.4
Larson, H.O.5
Levand, O.6
Weaver, W.M.7
-
10
-
-
42949121815
-
-
note
-
50 values >100 nM in the B-RAF kinase assay did not meet the criteria for progression though the remaining portions of our assay paradigm.
-
-
-
-
11
-
-
42949162833
-
-
note
-
18, Agilent HPLC). Standards of 100, 10, and 1 μM were prepared in DMSO to generate a standard curve. Compound concentrations were determined by extrapolating peak areas from the standard curve generated from a linear regression analysis in Graph Pad Prism (GraphPad Software, San Diego, CA). The calculated Log P values for compounds 17-19 are 3.13, 4.20, and 5.07, respectively.
-
-
-
-
12
-
-
42949091630
-
-
note
-
50 values for the sulfonamide analogs 14-16, the (NHMe) substituent still ranks favorably for displaying excellent B-RAF kinase inhibition (Table 1).
-
-
-
-
13
-
-
42949167021
-
-
note
-
a values of ∼5.8 versus ∼11.8 for the cyclopropyl analogs 17-19.
-
-
-
-
14
-
-
41649114134
-
-
Crawford S., Belajic D., Wei J., Riley J.P., Dunford P.J., Bembenek S., Fourie A., Edwards J.P., Karlsson L., Brunmark A., Wolin R.L., and Blevitt J.M. Mol. Can. Ther. 7 (2008) 492
-
(2008)
Mol. Can. Ther.
, vol.7
, pp. 492
-
-
Crawford, S.1
Belajic, D.2
Wei, J.3
Riley, J.P.4
Dunford, P.J.5
Bembenek, S.6
Fourie, A.7
Edwards, J.P.8
Karlsson, L.9
Brunmark, A.10
Wolin, R.L.11
Blevitt, J.M.12
-
15
-
-
42949133610
-
-
Upstate (Millipore) kinase panel. Millipore Corp. 290 Concord Rd. Billerica, MA 01821.
-
Upstate (Millipore) kinase panel. Millipore Corp. 290 Concord Rd. Billerica, MA 01821.
-
-
-
-
16
-
-
27944490693
-
-
Takle A.K., Brown M.J.B., Davies S., Dean D.K., Francis G., Gaiba A., Hird A.W., King F.D., Lovell P.J., Naylor A., Reith A.D., Steadman J.G., and Wilson D.M. Bioorg. Med. Chem. Lett. 16 (2006) 378
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 378
-
-
Takle, A.K.1
Brown, M.J.B.2
Davies, S.3
Dean, D.K.4
Francis, G.5
Gaiba, A.6
Hird, A.W.7
King, F.D.8
Lovell, P.J.9
Naylor, A.10
Reith, A.D.11
Steadman, J.G.12
Wilson, D.M.13
|