Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel

D. S. Su, A. Balog, D. Meng, P. Bertinato, S. J. Danishefsky, Y. H. Zheng, T. C. Chou, L. He, Susan Band Horwitz

Research output: Contribution to journalArticle

117 Citations (Scopus)

Abstract

Ahead! Epothilone B (1, R = Me) displayed better antitumor activity than paclitaxel (Taxol), as shown by in vivo studies with resistant mouse tumor models. The 'acyl sector' C1-C8 in the epothilones is very sensitive to modification. The other two sectors (see structure on the right) can be varied to a certain extent; however, none of the analogues examined thus far have surpassed the parent compound.

Original languageEnglish (US)
Pages (from-to)2093-2096
Number of pages4
JournalAngewandte Chemie - International Edition
Volume36
Issue number19
StatePublished - 1997

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Epothilones
Paclitaxel
Tumors

Keywords

  • Antitumor agents
  • Epothilones
  • In vivo testing
  • Natural products
  • Structure-activity relationships

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Su, D. S., Balog, A., Meng, D., Bertinato, P., Danishefsky, S. J., Zheng, Y. H., ... Band Horwitz, S. (1997). Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel. Angewandte Chemie - International Edition, 36(19), 2093-2096.

Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel. / Su, D. S.; Balog, A.; Meng, D.; Bertinato, P.; Danishefsky, S. J.; Zheng, Y. H.; Chou, T. C.; He, L.; Band Horwitz, Susan.

In: Angewandte Chemie - International Edition, Vol. 36, No. 19, 1997, p. 2093-2096.

Research output: Contribution to journalArticle

Su, DS, Balog, A, Meng, D, Bertinato, P, Danishefsky, SJ, Zheng, YH, Chou, TC, He, L & Band Horwitz, S 1997, 'Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel', Angewandte Chemie - International Edition, vol. 36, no. 19, pp. 2093-2096.
Su DS, Balog A, Meng D, Bertinato P, Danishefsky SJ, Zheng YH et al. Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel. Angewandte Chemie - International Edition. 1997;36(19):2093-2096.
Su, D. S. ; Balog, A. ; Meng, D. ; Bertinato, P. ; Danishefsky, S. J. ; Zheng, Y. H. ; Chou, T. C. ; He, L. ; Band Horwitz, Susan. / Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel. In: Angewandte Chemie - International Edition. 1997 ; Vol. 36, No. 19. pp. 2093-2096.
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