-
1
-
-
34250197079
-
-
Dutcher J.P., Novik Y., O'Boyle K., Marcoullis G., Secco C., and Wiernik P.H. J. Clin. Pharmacol. 40 (2000) 1097
-
(2000)
J. Clin. Pharmacol.
, vol.40
, pp. 1097
-
-
Dutcher, J.P.1
Novik, Y.2
O'Boyle, K.3
Marcoullis, G.4
Secco, C.5
Wiernik, P.H.6
-
4
-
-
0032190094
-
-
Ferhat L., Cook C., Chauviere M., Harper M., Kress M., Lyons G.E., and Baas P.W. J. Neurosci. 18 (1998) 7822
-
(1998)
J. Neurosci.
, vol.18
, pp. 7822
-
-
Ferhat, L.1
Cook, C.2
Chauviere, M.3
Harper, M.4
Kress, M.5
Lyons, G.E.6
Baas, P.W.7
-
5
-
-
0033615357
-
-
Mayer T.U., Kapoor T.M., Haggarty S.J., King R.W., Schreiber S.L., and Mitchison T.J. Science 286 (1999) 971
-
(1999)
Science
, vol.286
, pp. 971
-
-
Mayer, T.U.1
Kapoor, T.M.2
Haggarty, S.J.3
King, R.W.4
Schreiber, S.L.5
Mitchison, T.J.6
-
6
-
-
2342563857
-
-
Sakowicz R., Finer J.T., Beraud C., Crompton A., Lewis E., Fritsch A., Lee Y., Mak J., Moody R., Turincio R., Chabala J.C., Gonzales P., Roth S., Weitman S., and Wood K.W. Cancer Res. 64 (2004) 3276
-
(2004)
Cancer Res.
, vol.64
, pp. 3276
-
-
Sakowicz, R.1
Finer, J.T.2
Beraud, C.3
Crompton, A.4
Lewis, E.5
Fritsch, A.6
Lee, Y.7
Mak, J.8
Moody, R.9
Turincio, R.10
Chabala, J.C.11
Gonzales, P.12
Roth, S.13
Weitman, S.14
Wood, K.W.15
-
7
-
-
0034682703
-
-
Heald R. Cell 102 (2000) 399
-
(2000)
Cell
, vol.102
, pp. 399
-
-
Heald, R.1
-
12
-
-
20144388363
-
-
Cox C.D., Breslin M.J., Mariano B.J., Coleman P.J., Buser C.A., Walsh E.S., Hamilton K., Huber H.E., Kohl N.E., Torrent M., Yan Y., Kuo L.C., and Hartman G.D. Bioorg. Med. Chem. Lett. 15 (2005) 2041
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 2041
-
-
Cox, C.D.1
Breslin, M.J.2
Mariano, B.J.3
Coleman, P.J.4
Buser, C.A.5
Walsh, E.S.6
Hamilton, K.7
Huber, H.E.8
Kohl, N.E.9
Torrent, M.10
Yan, Y.11
Kuo, L.C.12
Hartman, G.D.13
-
13
-
-
33144468938
-
-
Fraley M.E., Garbaccio R.M., Arrington K.L., Hoffman W.F., Tasber E.S., Coleman P.J., Buser C.A., Walsh E.S., Hamilton K., Fernandes C., Schaber M.D., Lobell R.B., Tao W., South V.J., Yan Y., Kuo L.C., Prueksaritanont T., Shu C., Torrent M., Heimbrook D.C., Kohl N.E., Huber H.E., and Hartman G.D. Bioorg. Med. Chem. Lett. 16 (2006) 1775
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 1775
-
-
Fraley, M.E.1
Garbaccio, R.M.2
Arrington, K.L.3
Hoffman, W.F.4
Tasber, E.S.5
Coleman, P.J.6
Buser, C.A.7
Walsh, E.S.8
Hamilton, K.9
Fernandes, C.10
Schaber, M.D.11
Lobell, R.B.12
Tao, W.13
South, V.J.14
Yan, Y.15
Kuo, L.C.16
Prueksaritanont, T.17
Shu, C.18
Torrent, M.19
Heimbrook, D.C.20
Kohl, N.E.21
Huber, H.E.22
Hartman, G.D.23
more..
-
14
-
-
33144455399
-
-
Garbaccio R.M., Fraley M.E., Tasber E.S., Olson C.M., Hoffman W.F., Arrington K.L., Torrent M., Buser C.A., Walsh E.S., Hamilton K., Schaber M.D., Fernandes C., Lobell R.B., Tao W., South V.J., Yan Y., Kuo L.C., Prueksaritanont T., Slaughter D.E., Shu C., Heimbrook D.C., Kohl N.E., Huber H.E., and Hartman G.D. Bioorg. Med. Chem. Lett. 16 (2006) 1780
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 1780
-
-
Garbaccio, R.M.1
Fraley, M.E.2
Tasber, E.S.3
Olson, C.M.4
Hoffman, W.F.5
Arrington, K.L.6
Torrent, M.7
Buser, C.A.8
Walsh, E.S.9
Hamilton, K.10
Schaber, M.D.11
Fernandes, C.12
Lobell, R.B.13
Tao, W.14
South, V.J.15
Yan, Y.16
Kuo, L.C.17
Prueksaritanont, T.18
Slaughter, D.E.19
Shu, C.20
Heimbrook, D.C.21
Kohl, N.E.22
Huber, H.E.23
Hartman, G.D.24
more..
-
15
-
-
33646175956
-
-
Cox C.D., Torrent M., Breslin M.J., Mariano B.J., Whitman D.B., Coleman P.J., Buser C.A., Walsh E.S., Hamilton K., Schaber M.D., Lobell R.B., Tao W., South V.J., Kohl N.E., Yan Y., Kuo L.C., Prueksaritanont T., Slaughter D.E., Li C., Mahan E., Lu B., and Hartman G.D. Bioorg. Med. Chem. Lett. 16 (2006) 3175
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 3175
-
-
Cox, C.D.1
Torrent, M.2
Breslin, M.J.3
Mariano, B.J.4
Whitman, D.B.5
Coleman, P.J.6
Buser, C.A.7
Walsh, E.S.8
Hamilton, K.9
Schaber, M.D.10
Lobell, R.B.11
Tao, W.12
South, V.J.13
Kohl, N.E.14
Yan, Y.15
Kuo, L.C.16
Prueksaritanont, T.17
Slaughter, D.E.18
Li, C.19
Mahan, E.20
Lu, B.21
Hartman, G.D.22
more..
-
16
-
-
33644794320
-
-
Tarby C.M., Kaltenbach III R.F., Huynh T., Pudzianowski A., Shen H., Ortega-Nanos M., Sheriff S., Newitt J.A., McDonnell P.A., Burford N., Fairchild C.R., Vaccaro W., Chen Z., Borzilleri R.M., Naglich J., Lombardo L.J., Gottardis M., Trainor G.L., and Roussell D.L. Bioorg. Med. Chem. Lett. 16 (2006) 2095
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 2095
-
-
Tarby, C.M.1
Kaltenbach III, R.F.2
Huynh, T.3
Pudzianowski, A.4
Shen, H.5
Ortega-Nanos, M.6
Sheriff, S.7
Newitt, J.A.8
McDonnell, P.A.9
Burford, N.10
Fairchild, C.R.11
Vaccaro, W.12
Chen, Z.13
Borzilleri, R.M.14
Naglich, J.15
Lombardo, L.J.16
Gottardis, M.17
Trainor, G.L.18
Roussell, D.L.19
-
17
-
-
33745131839
-
-
Kim K.S., Lu S., Cornelius L.A., Lombardo L.J., Borzilleri R.M., Schroeder G.M., Sheng C., Rovnyak G., Crews D., Schmidt R.J., Williams D.K., Bhide R.S., Traeger S.C., McDonnell P.A., Mueller L., Sheriff S., Newitt J.A., Pudzianowski A.T., Yang Z., Wild R., Lee F.Y., Batorsky R., Ryder J.S., Ortega-Nanos M., Shen H., Gottardis M., and Roussell D.L. Bioorg. Med. Chem. Lett. 16 (2006) 3937
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 3937
-
-
Kim, K.S.1
Lu, S.2
Cornelius, L.A.3
Lombardo, L.J.4
Borzilleri, R.M.5
Schroeder, G.M.6
Sheng, C.7
Rovnyak, G.8
Crews, D.9
Schmidt, R.J.10
Williams, D.K.11
Bhide, R.S.12
Traeger, S.C.13
McDonnell, P.A.14
Mueller, L.15
Sheriff, S.16
Newitt, J.A.17
Pudzianowski, A.T.18
Yang, Z.19
Wild, R.20
Lee, F.Y.21
Batorsky, R.22
Ryder, J.S.23
Ortega-Nanos, M.24
Shen, H.25
Gottardis, M.26
Roussell, D.L.27
more..
-
19
-
-
25844479168
-
-
Sunder-Plassmann N., Sarli V., Gartner M., Utz M., Seiler J., Huemmer S., Mayer T.U., Surrey T., and Giannis A. Bioorg. Med. Chem. 13 (2005) 6094
-
(2005)
Bioorg. Med. Chem.
, vol.13
, pp. 6094
-
-
Sunder-Plassmann, N.1
Sarli, V.2
Gartner, M.3
Utz, M.4
Seiler, J.5
Huemmer, S.6
Mayer, T.U.7
Surrey, T.8
Giannis, A.9
-
20
-
-
34250206205
-
-
Gartner M., Mueller T., Simon J.C., Giannis A., and Sleeman J.P. Chem. Biol. Chem. 6 (2005) 1
-
(2005)
Chem. Biol. Chem.
, vol.6
, pp. 1
-
-
Gartner, M.1
Mueller, T.2
Simon, J.C.3
Giannis, A.4
Sleeman, J.P.5
-
21
-
-
22144463476
-
-
Gartner M., Sunder-Plassmann N., Seiler J., Utz M., Vernos I., Surrey T., and Giannis A. Chem. Biol. Chem. 6 (2005) 1173
-
(2005)
Chem. Biol. Chem.
, vol.6
, pp. 1173
-
-
Gartner, M.1
Sunder-Plassmann, N.2
Seiler, J.3
Utz, M.4
Vernos, I.5
Surrey, T.6
Giannis, A.7
-
22
-
-
27744596104
-
-
Sarli V., Huemmer S., Sunder-Plassmann N., Mayer T.U., and Giannis A. Chem. Biol. Chem. 6 (2005) 2005
-
(2005)
Chem. Biol. Chem.
, vol.6
, pp. 2005
-
-
Sarli, V.1
Huemmer, S.2
Sunder-Plassmann, N.3
Mayer, T.U.4
Giannis, A.5
-
27
-
-
34250175011
-
-
All final compounds displayed spectral data (NMR, MS) that were consistent with the assigned structure.
-
-
-
-
28
-
-
0037179635
-
-
Andersen H.S., Olsen O.H., Iversen L.F., Sorensen A.L.P., Mortensen S.B., Christensen M.S., Branner S., Hansen T.K., Lau J.F., Jeppesen L., Moran E.J., Su J., Bakir F., Judge L., Shahbaz M., Collins T., Vo T., Newman M.J., Ripka W.C., and Moller N.P.H. J. Med. Chem. 45 (2002) 4443
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4443
-
-
Andersen, H.S.1
Olsen, O.H.2
Iversen, L.F.3
Sorensen, A.L.P.4
Mortensen, S.B.5
Christensen, M.S.6
Branner, S.7
Hansen, T.K.8
Lau, J.F.9
Jeppesen, L.10
Moran, E.J.11
Su, J.12
Bakir, F.13
Judge, L.14
Shahbaz, M.15
Collins, T.16
Vo, T.17
Newman, M.J.18
Ripka, W.C.19
Moller, N.P.H.20
more..
-
29
-
-
34250178663
-
-
note
-
6-tagged) in 20 μl of assay buffer was dispensed to black 384-well assay plates. Compounds in DMSO and arrayed in 11 point 1/2 log dilution dose response (final top concentration of 96 μM, 1% DMSO in all assay wells) were added by passive pin transfer, followed by addition of 5 μl assay buffer containing taxol-stabilized bovine brain microtubules (Cytoskeleton) and ATP. The final concentrations of KSP, microtubules, and ATP were 15 nM, 500 nM, and 30 μM, respectively. After a 2-h room-temperature incubation, ADPQuest assay reagents were added according to the manufacturer's instructions, and the resulting fluorescence signal was read on a Molecular Devices Acquest plate reader. Raw fluorescence data were normalized to negative (DMSO) and positive (compound 2a, as a racemic mixture) controls. Data analysis was performed using Spotfire (v8.1, Spotfire, Inc.) and Kalypsys proprietary software.
-
-
-
-
30
-
-
34250194866
-
-
note
-
′) horseradish peroxidase conjugate (Jackson ImmunoResearch), and a chemiluminescent substrate (POD, Roche Applied Science). Signal detection, data normalization, and data analysis were similar to that in Ref. 9.
-
-
-
-
31
-
-
34250163436
-
-
note
-
5 cells/ml in medium with 1% fetal bovine serum. Compounds in DMSO and arrayed in 11 point 1/2 log dilution dose response (final top concentration of 96 μM, 1% DMSO in all assay wells) were added by passive pin transfer. After 60 h incubation, cell viability was measured by dispensing an equal volume of ATPLite reagent (Perkin-Elmer). Signal detection, data normalization, and data analysis were similar to that in Ref. 9.
-
-
-
-
32
-
-
34250169684
-
-
note
-
free = 0.208/0.272.
-
-
-
-
35
-
-
34250184045
-
-
note
-
Compound 33 was resolved using a Chiralpak IA column (4.6 mm × 250 mm) eluting 10% i-PrOH/90% heptane/0.1% TFA, 1 mL/min. The first eluting isomer showed ATPase activity of 0.48 μM versus 3.9 μM for the second eluting isomer. The absolute stereochemistry was not determined; the resolution of the crystal structure was not sufficient for definitive assignment.
-
-
-
-
36
-
-
34250222722
-
-
note
-
′) Alexa 488 (Invitrogen). Chromosomal DNA was stained with 4′-6-diamidino-2-phenylindole (DAPI, Sigma). Cells were imaged on a Zeiss Axiovert 2 with an ORCA-ER CCD camera (Hamamatsu) and OpenLab software (Improvision). Images were imported into Adobe Photoshop for labeling and minor alterations in contrast.
-
-
-
-
37
-
-
34250220901
-
-
note
-
A-549 cells in medium with 1% fetal bovine serum were treated with DMSO vehicle (<=0.15 % final) alone or containing compounds as specified for 18 h. To test reversibility of mitotic arrest, previously treated cells were washed three times with medium containing 1% fetal bovine serum and then replated in the same for an additional 24 h. Cells were harvested, washed twice with phosphate-buffered saline containing 2% fetal bovine serum, and then resuspended in 1 ml of the same wash buffer. For fixation, 3 ml of -20 °C absolute ethanol was added slowly, followed by a 1-h incubation on ice. Fixed cells were then washed twice with phosphate-buffered saline and resuspended in staining buffer (phosphate-buffered saline containing 3.8 mM sodium citrate, 50 μg/ml propidium iodide, and 100 μg/ml RNase A) for a minimum of 1 h at 4 °C. Cells were analyzed on a BD LSR flow cytometer.
-
-
-
-
39
-
-
22244459880
-
-
Tao W., South V.J., Zhang Y., Davide J.P., Farrell L., Kohl N.E., Sepp-Lorenzino L., and Lobell R.B. Cancer Cell 8 (2005) 49
-
(2005)
Cancer Cell
, vol.8
, pp. 49
-
-
Tao, W.1
South, V.J.2
Zhang, Y.3
Davide, J.P.4
Farrell, L.5
Kohl, N.E.6
Sepp-Lorenzino, L.7
Lobell, R.B.8
|