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


Authors: Su, D. S.; Balog, A.; Meng, D.; Bertinato, P.; Danishefsky, S. J.; Zheng, Y. H.; Chou, T. C.; He, L.; Horwitz, S. B.
Article Title: Structure-activity relationships of the epothilones and the first in vivo comparison with paclitaxel
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.
Keywords: antitumor agents; structure-activity relationships; epothilones; natural products; in vivo testing
Journal Title: Angewandte Chemie - International Edition
Volume: 36
Issue: 19
ISSN: 1433-7851
Publisher: Wiley Blackwell  
Date Published: 1997-10-17
Start Page: 2093
End Page: 2096
Language: English
PROVIDER: scopus
DOI: 10.1002/anie.199720931
DOI/URL:
Notes: Article -- Export Date: 17 March 2017 -- Source: Scopus
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  1. Aaron Balog
    14 Balog
  2. Ting-Chao Chou
    319 Chou
  3. Dongfang   Meng
    17 Meng
  4. Dai-Shi   Su
    12 Su