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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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(1993)
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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(1993)
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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Acc. Chem. Res.
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Reviews: Balkenhohl, F.; von dem Bussche-Hünnefeld, C.; Lansky, A.; Zechel, C. Angew. Chem. Int. Ed. Engl. 1996, 35, 2288. Gordon, E. M.; Gallop, M. A.; Patel, D. V. Acc. Chem. Res. 1996, 29, 144. Ellman, J. A. Acc. Chem. Res. 1996, 29, 132. Still, W. C. Acc. Chem. Res. 1996, 29, 155. Terrett, N. K.; Gardner, M.; Gordon, D. W.; Kobylecki, R. J.; Steele, J. Tetrahedron 1995, 51, 8135. Gallop, M. A.; Barrett, R. W.; Dower, W. J.; Fodor, S. P. A.; Gordon, E. M. J. Med. Chem. 1994, 37, 1233 and 1385. Janda, K. D. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 10779. Pavia, M. R.; Sawyer, T. K.; Moos, W. H. Bioorg. Med. Chem. Lett. 1993, 3, 387. Books and monographs: Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery; Chaiken, I. M., Janda, K. D., Eds.; ACS: Washington, 1996. Combinatorial Libraries - Synthesis, Screening, and Application Potential; Cortese, R., Ed.; Walter de Gruyter: New York, 1996. Symposium-in-Print: Bioorg. Med. Chem. Lett. 1993, 3, 381-476; Bioorg. Med. Chem. 1996, 4, 631-738; Acc. Chem. Res. 1996, 29, 112-170; Tetrahedron 1997, 53, 6573-6705; Chem. Rev. 1997, 97, 347-510; Tetrahedron 1998, 54, 3955-4150; Bioorg. Med. Chem. Lett. 1998, 8, in press.
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(1997)
Tetrahedron
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This reagent seems to be particularly efficient for coupling secondary amines, see:
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This reagent seems to be particularly efficient for coupling secondary amines, see: Richter, L. S.; Zuckerman, R. N. Bioorg. Med. Chem. Lett. 1995, 5, 1159. Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47.
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Richter, L.S.1
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0345329874
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Freshly activated and methanol-washed Dowex 50WX8-400 strongly acidic resin was used.
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Freshly activated and methanol-washed Dowex 50WX8-400 strongly acidic resin was used.
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113
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The use of three A amines additionally as B amines (B10, B12, and B13) in the 3×15 format produces three duplicate samples (i.e. 3×14 format, A2B10=A7B12, A2B13=A6B12, and A6B10=A7B13) which were not prepared twice, only once. This duplication was deliberate and was based on prior testing results in targets under investigation that identified their presence in lead structures.
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The use of three A amines additionally as B amines (B10, B12, and B13) in the 3×15 format produces three duplicate samples (i.e. 3×14 format, A2B10=A7B12, A2B13=A6B12, and A6B10=A7B13) which were not prepared twice, only once. This duplication was deliberate and was based on prior testing results in targets under investigation that identified their presence in lead structures.
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The tricarboxylic acids C31 and C32 are commercially available. Experimental details for the preparation of C33-C37 will be supplied upon request. Similarly, details of the % conversions (mg amounts) of products obtained from the deconvolution resynthesis, library syntheses, the tetramer libraries, A-scan, B-scan, and related studies has been compiled and is available upon request.
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The tricarboxylic acids C31 and C32 are commercially available. Experimental details for the preparation of C33-C37 will be supplied upon request. Similarly, details of the % conversions (mg amounts) of products obtained from the deconvolution resynthesis, library syntheses, the tetramer libraries, A-scan, B-scan, and related studies has been compiled and is available upon request.
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