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6
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0036605562
-
-
50 was determined with bovine brain FTase using the SPA assay, as in ref 10b.
-
50 was determined with bovine brain FTase using the SPA assay, as in ref 10b. Crul M., de Klerk G.J., Swart M., van't Veer L.J., de Jong D., Boerrigter L., Palmer P.A., Bol C.J., Tan H., de Gast G.C., Beijnen J.H., Schellens J.H.M. J. Clin. Oncol. 20:2002;2726.
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Tan, H.9
De Gast, G.C.10
Beijnen, J.H.11
Schellens, J.H.M.12
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7
-
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0034071688
-
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50 was determined with bovine brain FTase using the SPA assay, as in ref 10b.
-
50 was determined with bovine brain FTase using the SPA assay, as in ref 10b. Adjei A.A., Erlichman C., Davis J.N., Cutler D.L., Sloan J.A., Marks S., Hanson L.J., Svingen P.A., Atherton P., Bishop W.R., Kirschmeier P., Kaufmann S.H. Cancer Res. 60:2000;1871.
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8
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(a) Karp J.E., Kaufmann S.H., Adjei A.A., Lancet J.E., Wright J.J., End D.W. Curr. Opin. Oncol. 13:2001;470.
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11
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15144355763
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Rosenberg, S.14
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12
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0033539110
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(b) O'Connor S.J., Barr K.J., Wang L., Sorensen B.K., Tasker A.S., Sham H., Ng S., Cohen J., Devine E., Cherian S., Saeed B., Zhang H., Lee J.Y., Warner R., Tahir S., Kovar P., Ewing P., Alder J., Mitten M., Leal J., Marsh K., Bauch J., Hoffman D.J., Sebti S.M., Rosenberg S.H. J. Med. Chem. 42:1999;3701
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13
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0344822640
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(c) Henry K.J. Jr., Wasicak J., Tasker A.S., Cohen J., Ewing P., Mitten M., Larsen J.J., Kalvin D.M., Swenson R., Ng S., Saeed B., Cherian S., Sham H., Rosenberg S.H. J. Med. Chem. 42:1999;4844.
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Larsen, J.J.7
Kalvin, D.M.8
Swenson, R.9
Ng, S.10
Saeed, B.11
Cherian, S.12
Sham, H.13
Rosenberg, S.H.14
-
14
-
-
0033535420
-
-
(d) Shen W., Fakhoury S., Donner G., Henry K., Lee J., Zhang H., Cohen J., Warner R., Saeed B., Cherian S., Tahir S., Kovar P., Bauch J., Ng S., Marsh K., Sham H., Rosenberg S. Bioorg. Med. Chem. Lett. 9:1999;703.
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Warner, R.8
Saeed, B.9
Cherian, S.10
Tahir, S.11
Kovar, P.12
Bauch, J.13
Ng, S.14
Marsh, K.15
Sham, H.16
Rosenberg, S.17
-
15
-
-
0033583527
-
-
(e) Augeri D.J., Janowick D., Kalvin D., Sullivan G., Larsen J., Dickman D., Ding H., Cohen J., Lee J., Warner R., Kovar P., Cherian S., Saeed B., Zhang H., Tahir S., Ng S., Sham H., Rosenberg S.H. Bioorg. Med. Chem. Lett. 9:1998;1069.
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Warner, R.10
Kovar, P.11
Cherian, S.12
Saeed, B.13
Zhang, H.14
Tahir, S.15
Ng, S.16
Sham, H.17
Rosenberg, S.H.18
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16
-
-
85031209757
-
-
Unpublished data
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Wang, W. Unpublished data.
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Wang, W.1
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17
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0033594336
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Vasudevan A., Qian Y., Vogt A., Blaskovich M.A., Ohkanda J., Sebti S.M., Hamilton A.D. J. Med. Chem. 42:1999;1333.
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Sebti, S.M.6
Hamilton, A.D.7
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18
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-
0030984431
-
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For a similar conversion, aniline to methyl benzoate via diazotization/iodination followed by palladium catalyzed carbomethoxylation, see:
-
For a similar conversion, aniline to methyl benzoate via diazotization/iodination followed by palladium catalyzed carbomethoxylation, see: Diaz P., Michel S., Stella L., Charpentier B. Bioorg. Med. Chem. Lett. 7:1997;2289.
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Abdel-Magid A.F., Carson K.G., Harris B.D., Maryanoff C.A., Shah R.D. J. Org. Chem. 61:1996;3849.
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Shah, R.D.5
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22
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85031201030
-
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note
-
1H NMR, mass spectroscopy and elemental analysis.
-
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23
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0030034763
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Hunt J.T., Lee V.G., Leftheris K., Seizinger B., Carboni J., Mabus J., Ricca C., Yan N., Manne V. J. Med. Chem. 39:1996;353.
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Yan, N.8
Manne, V.9
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24
-
-
85031197936
-
-
note
-
50 data were determined against FTase and GGTase1 (purified from bovine brain) using the scintillation proximity assay (SPA). The compounds were assayed once and the reliability of the assay was±50%. See ref 10b for further details.
-
-
-
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25
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0033584194
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(a) Ciccarone T.M., MacTough S.C., Williams T.M., Dinsmore C.J., O'Neill T.J., Shah D., Culberson J.C., Koblan K.S., Kohl N.E., Gibbs J.B., Oliff A.I., Graham S.L., Hartman G.D. Bioorg. Med. Chem. Lett. 9:1999;1991.
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Shah, D.6
Culberson, J.C.7
Koblan, K.S.8
Kohl, N.E.9
Gibbs, J.B.10
Oliff, A.I.11
Graham, S.L.12
Hartman, G.D.13
-
26
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0033530870
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(b) Dinsmore C.J., Williams T.M., O'Neill T.J., Liu D., Rands E., Culberson J.C., Lobell R.B., Koblan K.S., Kohl N.E., Gibbs J.B. Bioorg. Med. Chem. Lett. 9:1999;3301.
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Dinsmore, C.J.1
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Culberson, J.C.6
Lobell, R.B.7
Koblan, K.S.8
Kohl, N.E.9
Gibbs, J.B.10
-
27
-
-
85031198416
-
-
note
-
Subconfluent NIH3T3 ras-transformed cells were used for the Ha-Ras processing assay. The compounds were assayed once and the reliability of the assay was ±50-100%. See ref 10b for further details.
-
-
-
-
28
-
-
85031205153
-
-
note
-
(a) Crystals of rat farnesyltransferase were exposed to compound stabilization solutions for approximately four hours before data collection Diffraction data was collected on a rotating anode source, and a Mar-135 CCD camera system. Data reduction using the HKL2000 program suite yielded a data set which was 98% complete to 2.8 Å, with merging R-values of 4.8% overall. Electron density maps were calculated from models which had been rigid body refined against the data. Models were constructed to fit the observed electron density, and were refined using the XPLOR program package. Final models have R work and R-free values of 24.9 and 32.1% respectively, with no water molecules. Models of this complex have been submitted to the Protein Data Bank (accession 1NL4). (b) Muchmore, S. Unpublished data.
-
-
-
-
29
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0033578085
-
-
For the X-ray crystal structure of 2 with FTase/FPP, see:
-
For the X-ray crystal structure of 2 with FTase/FPP, see: Strickland C.L., Weber P.C., Windsor W.T., Wu Z., Le H.V., Albanese M.M., Alvarez C.S., Cesarz D., del Rosario J., Deskus J., Mallams A.K., Njoroge F.G., Piwinski J.J., Remiszewski S., Rossman R.R., Tavera A.G., Vibulbhan B., Doll R.J., Girijavallabhan V.M., Ganguly A.K. J. Med. Chem. 42:1999;2125.
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Le, H.V.5
Albanese, M.M.6
Alvarez, C.S.7
Cesarz, D.8
Del Rosario, J.9
Deskus, J.10
Mallams, A.K.11
Njoroge, F.G.12
Piwinski, J.J.13
Remiszewski, S.14
Rossman, R.R.15
Tavera, A.G.16
Vibulbhan, B.17
Doll, R.J.18
Girijavallabhan, V.M.19
Ganguly, A.K.20
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