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27844467217
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note
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For selected examples of 1,4-benzodiazepine therapeutic agents or promising drug candidates see: (a) Anxiolytic, anticonvulsant, and antihypnotic agents, ref. 5.
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7
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(b) Selective cholecystokinin (CCK) receptor subtype A or B antagonists, Bock M. G., Dipardo R. M., Evans B. E., Rittle K. E., Whitter W. L., Veber D. F., Anderson P. S., Freidinger R. M., J. Med. Chem., 1989, 32, 13.
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Veber, D.F.6
Anderson, P.S.7
Freidinger, R.M.8
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8
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0019972014
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(c) κ-selective opioid antagonists, Römer D., Buscher H. H., Hill R. C., Maurer R., Petcher T. J., Zeugner H., Benson W., Finner E., Milkowski W., Thies P. W., Nature, 1982, 298, 759.
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Römer, D.1
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Maurer, R.4
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Zeugner, H.6
Benson, W.7
Finner, E.8
Milkowski, W.9
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(d) Platelet activating factor antagonists, Kornecki E., Ehrlich Y. H., Lenox R. H., Science, 1984, 226, 1454.
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27844469109
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Int. Pat. Appl., WO 93/00095, 1993
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(e) GPIIbIIIa inhibitors, Bondinell W. E., Callahan J. F., Huffman W. F., Keenan R. M., Ku T. W.-F., Newlander K. A., Int. Pat. Appl., WO 93/00095, 1993.
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Bondinell, W.E.1
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Ku, T.W.-F.5
Newlander, K.A.6
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11
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0027323459
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(f) Ras farnesyl transferase inhibitors, James G. L., Goldstein J. L., Brown M. S., Rawson T. E., Somers T. C., McDowell R. S., Crowley C. W., Lucas B. K., Levinson A. D., Marsters Jr. J. C., Science, 1993, 260, 1937.
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James, G.L.1
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Somers, T.C.5
McDowell, R.S.6
Crowley, C.W.7
Lucas, B.K.8
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(b) Bunin B. A., Plunkett M. J., Ellman J. A., Proc. Natl. Acad. Sci. USA, 1994, 91, 4708.
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Bunin, B.A.1
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Pavia, M.R.6
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Synthesis of the 1,4-benzodiazepine-2,5-dione class: (a) Boojamra C. G., Burow K. A., Ellman J. A., J. Org. Chem., 1995, 60, 5700.
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Boojamra, C.G.1
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Ellman, J.A.3
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17
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0028928237
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We have developed a more versatile synthesis strategy where the 2-aminobenzophenone is synthesized on the solid support. Plunkett M. J., Ellman J. A., J. Am. Chem. Soc., 1995, 117, 3306.
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0029952270
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This strategy has been used to construct a library of 11,200 compounds: Bunin B. A., Plunkett M. J., Ellman J. A., Methods in Enzymology, 1996, 267, 448-465.
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Bunin, B.A.1
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Ellman, J.A.3
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19
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33751156625
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We have developed a method to employ a silyl linkage where the compound is cleaved from the support by protodesilylation to provide no trace of the solid-phase synthesis sequence. Plunkett M. J., Ellman J. A., J. Org. Chem., 1995, 60, 6006.
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0025893762
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While our libraries synthesized to date have been made using the Geysen pin apparatus, our development of solid-phase synthesis methods has generally been performed on crosslinked aminomethyl polystyrene resin. Because optimization has been performed on gel-form resin, these synthetic methods may readily be adapted to a library synthesized with a split-and-mix approach first reported by Furka. Furka A., Sebestyen F., Asgedom M., Dibo G., Int. J. Peptide Protein Res., 1991, 37, 487.
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27
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27844542789
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As determined by the ninhydrin test
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As determined by the ninhydrin test.
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28
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27844442235
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Glycine was the only achiral amino acid used in the synthesis
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Glycine was the only achiral amino acid used in the synthesis.
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29
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27844596286
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M. D. Anderson Cancer Institute, Houston, TX, unpublished results
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Buddie R. A., Levin V., and coworkers, M. D. Anderson Cancer Institute, Houston, TX, unpublished results, 1995.
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(1995)
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Buddie, R.A.1
Levin, V.2
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30
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27844575208
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University of Michigan, unpublished results
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Glick G., and coworkers, University of Michigan, unpublished results, 1995.
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(1995)
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Glick, G.1
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31
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27844457604
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note
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These compounds have been synthesized on solid support because this provides the fastest, least expensive route for the synthesis of moderate amounts of compound.
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