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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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Fairchild, C.R.9
Long, B.H.10
Vite, G.D.11
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7
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0037425543
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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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12444300592
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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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Sinha, S.C.1
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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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Giannakakou, P.10
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For recent examples of syntheses of novel epothilone analogues, see: a) A. Regueiro-Ren, K. Leavitt, S.-H. Kim, G. Höfle, M. Kiffe, J. Z. Gougoutas, J. D. DiMarco, F. Y. F. Lee, C. R. Fairchild, B. H. Long, G. D. Vite, Org. Lett. 2002, 4, 3815; b) R. E. Taylor, Y. Chen, A. Beatty, D. C. Myles, Y. Zhou, J. Am. Chem. Soc. 2003, 125, 27; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; c) S. C. Sinha, J. Sun, Angew. Chem. 2002, 114, 1439; Angew. Chem. Int. Ed. 2002, 41, 1381; d) K. C. Nicolaou, A. Ritzén, K. Namoto, R. M. Buey, J. F. Diaz, J. M. Andreu, M. Wartmann, K. H. Altmann, A. O'Brate, P. Giannakakou, Tetrahedron 2002, 58, 6413; e) J. W. Bode, E. M. Carreira, J. Org. Chem. 2001, 66, 6410.
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For more information about clinical trials of dEpoB, visit: www.kosan.com.
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b) for the interfacing of these findings with earlier claims, see: J. D. White, R. G. Carter, K. F. Sundermann, M. Wartmann, J. Am. Chem. Soc. 2001, 123, 5407, and references in [8a].
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12444260099
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note
-
The terms α and β epoxidation anticipate the stereostructure of the products presented in structures 4 and 5.
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29
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0034684787
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It remains to be established whether this remarkable level of potency can be translated to achieve clinically useful therapeutic margins; for recent examples of alternative highly potent epothilone analogues, see: a) K. H. Altmann, G. Bold, G. Caravatti, A. Flörsheimer, V. Guagnano, M. Wartmann, Bioorg. Med. Chem. Lett. 2000, 10, 2765; b) K. C. Nicolaou, R. Scarpelli, B. Bollbuck, B. Werschkun, M. M. A. Pereira, M. Wartmann, K.-H. Altmann, D. Zaharevitz, R. Gussio, P. Giannakakou, Chem. Biol. 2000, 7, 593.
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Wartmann, M.6
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0033826818
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It remains to be established whether this remarkable level of potency can be translated to achieve clinically useful therapeutic margins; for recent examples of alternative highly potent epothilone analogues, see: a) K. H. Altmann, G. Bold, G. Caravatti, A. Flörsheimer, V. Guagnano, M. Wartmann, Bioorg. Med. Chem. Lett. 2000, 10, 2765; b) K. C. Nicolaou, R. Scarpelli, B. Bollbuck, B. Werschkun, M. M. A. Pereira, M. Wartmann, K.-H. Altmann, D. Zaharevitz, R. Gussio, P. Giannakakou, Chem. Biol. 2000, 7, 593.
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Gussio, R.9
Giannakakou, P.10
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