-
1
-
-
0001874067
-
-
O'Brien, R. D., Ed.; Plenum: New York
-
(a) Ariëns, E. J.; Beld, A. J.; Rodrigues de Miranda, J. F.; Simonis, A. M. In The Receptors: A Comprehensive Treatise; O'Brien, R. D., Ed.; Plenum: New York, 1979; pp 33-91.
-
(1979)
The Receptors: A Comprehensive Treatise
, pp. 33-91
-
-
Ariëns, E.J.1
Beld, A.J.2
Rodrigues De Miranda, J.F.3
Simonis, A.M.4
-
3
-
-
0346560160
-
-
World Patent WO 0242296, May 30, 2002
-
Farnesyl transferase: (a) Angibaud, P. R.; Venet, M. G.; Poncelet, V. S. ; World Patent WO 0242296, May 30, 2002.
-
-
-
Angibaud, P.R.1
Venet, M.G.2
Poncelet, V.S.3
-
4
-
-
0347190169
-
-
World Patent WO 0181322, November 1, 2001
-
(b) Ding, C. Z.; Hunt, J. T.; Leftheris, K.; Bhide, R. S. World Patent WO 0181322, November 1, 2001.
-
-
-
Ding, C.Z.1
Hunt, J.T.2
Leftheris, K.3
Bhide, R.S.4
-
5
-
-
0346560158
-
-
World Patent WO 9918951, April 22, 1999
-
(c) Ding, C. Z.; Hunt, J. T.; Leftheris, K.; Bhide, R. S. World Patent WO 9918951, April 22, 1999.
-
-
-
Ding, C.Z.1
Hunt, J.T.2
Leftheris, K.3
Bhide, R.S.4
-
7
-
-
0346560159
-
-
World Patent WO 9736879, October 9, 1997
-
(e) Graham, S. L.; Anthony, N. J.; Wai, J. S. World Patent WO 9736879, October 9, 1997.
-
-
-
Graham, S.L.1
Anthony, N.J.2
Wai, J.S.3
-
8
-
-
0347190168
-
-
World Patent WO 9730992, August 28, 1997
-
(f) Ding, C. Z.; Hunt, J. T.; Kim, S.; Mitt, T.; Bhide, R. S.; Leftheris, K. World Patent WO 9730992, August 28, 1997.
-
-
-
Ding, C.Z.1
Hunt, J.T.2
Kim, S.3
Mitt, T.4
Bhide, R.S.5
Leftheris, K.6
-
9
-
-
0345929068
-
-
World Patent WO 9532191, November 30, 1995
-
(g) Graham, S. L.; Anthony, N. J.; Wai, J. S. World Patent WO 9532191, November 30, 1995.
-
-
-
Graham, S.L.1
Anthony, N.J.2
Wai, J.S.3
-
10
-
-
9144263323
-
-
World Patent WO 9426723, November 24, 1994
-
(h) Marsters, J. C., Jr.; Brown, M. S.; Crowley, C. W.; Goldstein, J. L. ; James, G. L.; Macdowell, R. S.; Oare, D.; Rawson, T. E.; Reynolds, M.; Somers, T. G. World Patent WO 9426723, November 24, 1994.
-
-
-
Marsters Jr., J.C.1
Brown, M.S.2
Crowley, C.W.3
Goldstein, J.L.4
James, G.L.5
Macdowell, R.S.6
Oare, D.7
Rawson, T.E.8
Reynolds, M.9
Somers, T.G.10
-
11
-
-
0027191479
-
-
Reverse transcriptase
-
(i) Ripka, W. C.; De Lucca, G. V.; Bach, A. C., II; Pottorf, R. S.; Blaney, J. M. Tetrahedron 1993, 49, 3593. Reverse transcriptase:
-
(1993)
Tetrahedron
, vol.49
, pp. 3593
-
-
Ripka, W.C.1
De Lucca, G.V.2
Bach II, A.C.3
Pottorf, R.S.4
Blaney, J.M.5
-
12
-
-
0025740266
-
-
(j) Hargrave, D. K.; Proudfoot, J. R.; Grozinger, K. G.; Cullen, E.; Kapadia, S. R.; Patel, U. R.; Fuchs, V. U.; Mauldin, S. C.; Vitous, J.; Behnke, M. L.; Klunder, J. M.; Pal, K.; Skiles, J. W.; McNeil, D. W.; Rose, J. M.; Chow, G. C.; Skoog, M. T.; Wu, J. C.; Schmidt, G.; Engel, W. W.; Eberlein, W. G.; Saboe, T. D.; Campbell, S. J.; Rosenthal, A. S.; Adams, J. J. Med. Chem. 1991, 34, 2231.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2231
-
-
Hargrave, D.K.1
Proudfoot, J.R.2
Grozinger, K.G.3
Cullen, E.4
Kapadia, S.R.5
Patel, U.R.6
Fuchs, V.U.7
Mauldin, S.C.8
Vitous, J.9
Behnke, M.L.10
Klunder, J.M.11
Pal, K.12
Skiles, J.W.13
McNeil, D.W.14
Rose, J.M.15
Chow, G.C.16
Skoog, M.T.17
Wu, J.C.18
Schmidt, G.19
Engel, W.W.20
Eberlein, W.G.21
Saboe, T.D.22
Campbell, S.J.23
Rosenthal, A.S.24
Adams, J.25
more..
-
13
-
-
0025679303
-
-
(k) Merluzzi, V. J.; Hargrave, K. D.; Labadia, M.; Grozinger, K.; Skoog, M.; Wu, J. C.; Shih, C.-K.; Eckner, K.; Hattox, S.; Adams, J.; Rosenthal, A. S. ; Faanes, R.; Eckner, R. J.; Koup, R. A.; Sullivan, J. L. Science 1990, 250, 1411-1413.
-
(1990)
Science
, vol.250
, pp. 1411-1413
-
-
Merluzzi, V.J.1
Hargrave, K.D.2
Labadia, M.3
Grozinger, K.4
Skoog, M.5
Wu, J.C.6
Shih, C.-K.7
Eckner, K.8
Hattox, S.9
Adams, J.10
Rosenthal, A.S.11
Faanes, R.12
Eckner, R.J.13
Koup, R.A.14
Sullivan, J.L.15
-
14
-
-
0347820449
-
-
World Patent WO 0230912, April 18, 2002
-
γ-Secretase: (l) Churcher, I.; Nadin, A. J.; Owens, A. P. World Patent WO 0230912, April 18, 2002.
-
-
-
Churcher, I.1
Nadin, A.J.2
Owens, A.P.3
-
15
-
-
0031845332
-
-
Salata, J. J.; Jurkiewicz, N. K.; Wang, J.; Evans, B. E.; Orme, H. T.; Sanguinetti, M. C. Mol. Pharmacol. 1998, 53, 220.
-
(1998)
Mol. Pharmacol.
, vol.53
, pp. 220
-
-
Salata, J.J.1
Jurkiewicz, N.K.2
Wang, J.3
Evans, B.E.4
Orme, H.T.5
Sanguinetti, M.C.6
-
16
-
-
0034687226
-
-
(a) Liu, J.; Underwood, D. J.; Cascieri, M. A.; Rohrer, S. P.; Cantin, L.-D.; Chicchi, G.; Smith, A. B., III; Hirschmann, R. J. Med. Chem. 2000, 43, 3827-3831.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 3827-3831
-
-
Liu, J.1
Underwood, D.J.2
Cascieri, M.A.3
Rohrer, S.P.4
Cantin, L.-D.5
Chicchi, G.6
Smith III, A.B.7
Hirschmann, R.8
-
17
-
-
0027857964
-
-
(b) Hirschmann, R.; Nicolaou, K. C.; Piettranico, S.; Leahy, E. M.; Arison, B.; Cichy, M. A.; Spoors, P. G.; Shakespeare, W. C.; Sprengeler, P. A.; Hamley, P.; Smith, A. B., III; Reisine, T.; Raynor, K.; Maechler, L.; Donaldson, C.; Vale, W.; Freidinger, R. M.; Cascieri, M. R.; Strader, C. D. J. Am. Chem. Soc. 1993, 115, 12550-12568.
-
(1993)
J. Am. Chem. Soc.
, vol.115
, pp. 12550-12568
-
-
Hirschmann, R.1
Nicolaou, K.C.2
Piettranico, S.3
Leahy, E.M.4
Arison, B.5
Cichy, M.A.6
Spoors, P.G.7
Shakespeare, W.C.8
Sprengeler, P.A.9
Hamley, P.10
Smith III, A.B.11
Reisine, T.12
Raynor, K.13
Maechler, L.14
Donaldson, C.15
Vale, W.16
Freidinger, R.M.17
Cascieri, M.R.18
Strader, C.D.19
-
18
-
-
0347820447
-
-
Manuscript in preparation
-
(c) McVaugh, C.; Savinov, S.; Prasad, V.; Smith, A. B., III; Hirschmann, R. Manuscript in preparation.
-
-
-
McVaugh, C.1
Savinov, S.2
Prasad, V.3
Smith III, A.B.4
Hirschmann, R.5
-
19
-
-
0038754828
-
-
and references cited
-
Prasad, V.; Birzin, E. T.; McVaugh, C. T.; van Rijn, R. D.; Rohrer, S. P.; Chicchi, G.; Underwood, D. J.; Thornton, E. R.; Smith, A. B., III; Hirschmann, R. J. Med. Chem. 2003, 46, 1858-1869 and references cited.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1858-1869
-
-
Prasad, V.1
Birzin, E.T.2
McVaugh, C.T.3
Van Rijn, R.D.4
Rohrer, S.P.5
Chicchi, G.6
Underwood, D.J.7
Thornton, E.R.8
Smith III, A.B.9
Hirschmann, R.10
-
20
-
-
0347190167
-
-
Ph.D. Dissertation, University of Pennsylvania. We are indebted to Dr. Carl DeCicco, BristolMyers Squibb, for this information.
-
Prasad, V. Ph.D. Dissertation, University of Pennsylvania, 2001. We are indebted to Dr. Carl DeCicco, BristolMyers Squibb, for this information.
-
(2001)
-
-
Prasad, V.1
-
21
-
-
0345929065
-
-
note
-
Thus, the target of cortrisol is the glucocorticoid receptor, but it activates also the mineralocorticoid receptor. The reverse is true of aldosterone, which targets primarily the latter receptor. Interestingly, the manmade 1-dehydrocortisol (prednisolone) is more selective than cortisol.
-
-
-
-
22
-
-
0031152053
-
-
Spaller, M. R.; Burger, M. T.; Fardis, M.; Bartlett, P. A. Curr. Opin. Chem. Biol. 1997, 1, 47-53.
-
(1997)
Curr. Opin. Chem. Biol.
, vol.1
, pp. 47-53
-
-
Spaller, M.R.1
Burger, M.T.2
Fardis, M.3
Bartlett, P.A.4
-
23
-
-
0035810408
-
-
Abrous, L.; Hynes, J., Jr.; Friedrich, S. R.; Smith, A. B., III; Hirschmann, R. Org. Lett. 2001, 3, 1089-1092.
-
(2001)
Org. Lett.
, vol.3
, pp. 1089-1092
-
-
Abrous, L.1
Hynes Jr., J.2
Friedrich, S.R.3
Smith III, A.B.4
Hirschmann, R.5
-
25
-
-
0347820445
-
-
note
-
2O).
-
-
-
-
26
-
-
15444347630
-
-
Hirschmann, R.; Hynes, J., Jr.; Cichy-Knight, M. A.; van Rijn, R. D.; Sprengeler, P. A.; Spoors, P. G.; Shakespeare, W. C.; Pietranico-Cole, S.; Barbosa, J.; Liu, J.; Yao, W.; Rohrer, S.; Smith, A. B., III. J. Med. Chem. 1998, 41, 1382-1391.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 1382-1391
-
-
Hirschmann, R.1
Hynes Jr., J.2
Cichy-Knight, M.A.3
Van Rijn, R.D.4
Sprengeler, P.A.5
Spoors, P.G.6
Shakespeare, W.C.7
Pietranico-Cole, S.8
Barbosa, J.9
Liu, J.10
Yao, W.11
Rohrer, S.12
Smith III, A.B.13
-
27
-
-
0346560157
-
-
Ph.D. Dissertation, University Of Pennsylvania
-
Hynes, J., Jr. Ph.D. Dissertation, University of Pennsylvania, 1996.
-
(1996)
-
-
Hynes Jr., J.1
-
28
-
-
0346560156
-
-
note
-
We are indebted to Dr. Carl DeCicco, then at DuPont Pharmaceuticals, for helpful discussions.
-
-
-
-
29
-
-
0021763098
-
-
Midoux, P.; Grivet, J. P.; Delmotte, F.; Monsigny, M. Biochem. Biophys. Res. Comm. 1984, 119, 603.
-
(1984)
Biochem. Biophys. Res. Comm.
, vol.119
, pp. 603
-
-
Midoux, P.1
Grivet, J.P.2
Delmotte, F.3
Monsigny, M.4
-
32
-
-
0347820444
-
-
note
-
See the Supporting Information for more details.
-
-
-
-
33
-
-
0028804965
-
-
Prepared by reaction of commercially available pyrazine-2-carboxylic acid with thionyl chloride in benzene at reflux and purified by sublimation. Cynamon, M. H.; Gimi, R.; Gyenes, F.; Sharpe, C. A.; Bergmann, K. E.; Han, H. J.; Gregor, L. B.; Rapolu, R.; Luciano, G.; Welch, J. T. J. Med. Chem. 1995, 38, 3902.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 3902
-
-
Cynamon, M.H.1
Gimi, R.2
Gyenes, F.3
Sharpe, C.A.4
Bergmann, K.E.5
Han, H.J.6
Gregor, L.B.7
Rapolu, R.8
Luciano, G.9
Welch, J.T.10
-
34
-
-
33751385862
-
-
Ishihara, K.; Kurihara, H.; Yamamoto, H. J. Org. Chem. 1993, 58, 3791.
-
(1993)
J. Org. Chem.
, vol.58
, pp. 3791
-
-
Ishihara, K.1
Kurihara, H.2
Yamamoto, H.3
-
35
-
-
0345929064
-
-
note
-
In addition to providing a diverse collection of compounds for broad screening, exploring the synthesis of mixed diacyl derivatives will address the important chemical question of stability to acyl migration.
-
-
-
-
36
-
-
0032555443
-
-
Raman, P.; Stokes, S. S.; Angell, Y. M.; Flentke, G. R.; Rich, D. H. J. Org. Chem., 1998, 63, 5734-5735.
-
(1998)
J. Org. Chem.
, vol.63
, pp. 5734-5735
-
-
Raman, P.1
Stokes, S.S.2
Angell, Y.M.3
Flentke, G.R.4
Rich, D.H.5
-
37
-
-
0347820439
-
-
Process for Preparing Carbamates. European Patent EP0967199, 1999
-
Berrier, J. V. Process for Preparing Carbamates. European Patent EP0967199, 1999.
-
-
-
Berrier, J.V.1
-
38
-
-
0345929063
-
-
note
-
2O) after 2 h.
-
-
-
-
40
-
-
0002776196
-
-
(b) Boons, G.-J.; Castle, G. H.; Clase, J. A.; Grice, P.; Ley, S. V.; Pinel, C. Synlett 1993, 913.
-
(1993)
Synlett
, pp. 913
-
-
Boons, G.-J.1
Castle, G.H.2
Clase, J.A.3
Grice, P.4
Ley, S.V.5
Pinel, C.6
-
41
-
-
0000644801
-
-
Doyle, M. P.; Dellaria, J. F., Jr.; Siegfried, B.; Bishop, S. W. J. Org. Chem. 1977, 42, 3494.
-
(1977)
J. Org. Chem.
, vol.42
, pp. 3494
-
-
Doyle, M.P.1
Dellaria Jr., J.F.2
Siegfried, B.3
Bishop, S.W.4
-
42
-
-
0000249892
-
-
Doyle, M. P.; Siegfried, B.; Dellaria, J. F., Jr. J. Org. Chem. 1977, 42, 2426.
-
(1977)
J. Org. Chem.
, vol.42
, pp. 2426
-
-
Doyle, M.P.1
Siegfried, B.2
Dellaria Jr., J.F.3
-
45
-
-
0347820403
-
-
Ph.D. Dissertation, University of Pennsylvania
-
Cichy-Knight, M. Ph.D. Dissertation, University of Pennsylvania, 1997.
-
(1997)
-
-
Cichy-Knight, M.1
-
46
-
-
0347190163
-
-
note
-
Under chemical ionization (CI) conditions, a molecular ion having the same mass-to-charge ratio as the desired product was observed. Under electrospray ionization (ESI) conditions, a molecular ion corresponding to dimer formation was observed under both positive and negative ionization conditions. Signals corresponding to dimerization of molecules in the mass spectrometer is not uncommon under ESI conditions.
-
-
-
-
47
-
-
0347190162
-
-
note
-
Details regarding the preparation of compound (+)-100 are presented in the Supporting Information.
-
-
-
-
48
-
-
0346560120
-
-
note
-
Even under conditions of very high dilution (c = 0.001 N), only dimer formation was observed.
-
-
-
-
49
-
-
0345929062
-
-
note
-
Monte Carlo conformational searches were performed on MacroModel Version 6.0, using the MM2 force field and the Polak-Ribiere conjugate gradient as algorithm.
-
-
-
-
50
-
-
0347190138
-
-
note
-
We also synthesized the glucosamine derivative (-)-103, which afforded the macrocycle (-)-104 on treatment with potassium carbonate in DMF. Similarly, (-)-108 gave only the dimeric (+)-109 under conditions of high dilution. For details, see the Supporting Information.
-
-
-
-
51
-
-
0032503605
-
-
Scherer, G.; Kramer, M. L.; Schutkowski, M.; Reimer, U.; Fischer, G. J. Am. Chem. Soc. 1998, 120, 5568-5574.
-
(1998)
J. Am. Chem. Soc.
, vol.120
, pp. 5568-5574
-
-
Scherer, G.1
Kramer, M.L.2
Schutkowski, M.3
Reimer, U.4
Fischer, G.5
-
52
-
-
0030473242
-
-
Beausoleil, E.; L'Archevêque, B.; Bélec, L.; Atfani, M.; Lubell, W. D. J. Org. Chem. 1996, 61, 9447-54.
-
(1996)
J. Org. Chem.
, vol.61
, pp. 9447-9454
-
-
Beausoleil, E.1
L'Archevêque, B.2
Bélec, L.3
Atfani, M.4
Lubell, W.D.5
-
56
-
-
0019862208
-
-
(a) Veber, D. F.; Freidinger, R. M.; Perlow, D. S.; Paleveda, W. J.; Holly, F. W.; Strachan, R. G.; Nutt, R. F.; Arison, B. H.; Homnick, C.; Randall, W. C.; Glitzer, M. S.; Saperstein, R.; Hirschmann, R. Nature 1981, 292, 55.
-
(1981)
Nature
, vol.292
, pp. 55
-
-
Veber, D.F.1
Freidinger, R.M.2
Perlow, D.S.3
Paleveda, W.J.4
Holly, F.W.5
Strachan, R.G.6
Nutt, R.F.7
Arison, B.H.8
Homnick, C.9
Randall, W.C.10
Glitzer, M.S.11
Saperstein, R.12
Hirschmann, R.13
-
57
-
-
9144258768
-
-
(b) Veber, D. F.; Saperstein, R.; Nutt, R. F.; Freidinger, R. M.; Brady, S. F.; Curley, P.; Perlow, D. S.; Paleveda, W. J.; Colton, C. D.; Zacchei, A. G.; Tocco, D. J.; Hoff, D. R.; Vandlen, R. L.; Gerich, J. E.; Hall, L.; Mandarino, L.; Cordes, E. H.; Anderson, P. S.; Hirschmann, R. Life Sci. 1984, 34, 371.
-
(1984)
Life Sci.
, vol.34
, pp. 371
-
-
Veber, D.F.1
Saperstein, R.2
Nutt, R.F.3
Freidinger, R.M.4
Brady, S.F.5
Curley, P.6
Perlow, D.S.7
Paleveda, W.J.8
Colton, C.D.9
Zacchei, A.G.10
Tocco, D.J.11
Hoff, D.R.12
Vandlen, R.L.13
Gerich, J.E.14
Hall, L.15
Mandarino, L.16
Cordes, E.H.17
Anderson, P.S.18
Hirschmann, R.19
-
58
-
-
0000985034
-
-
It is relevant to note that Schultz and co-workers reported a convenient method for the preparation of macrocycles via the bimolecular cyclization of o-fluorobenzamides; this protocol failed with the corresponding tertiary amide, affording the undesired unimolecular reaction products: Schultz, A. G.; Pinto, D. J. P.; Welch, M.; Kullnig, R. K. J. Org. Chem. 1988, 53, 1372-1380.
-
(1988)
J. Org. Chem.
, vol.53
, pp. 1372-1380
-
-
Schultz, A.G.1
Pinto, D.J.P.2
Welch, M.3
Kullnig, R.K.4
|