| Autor: |
Barboni, L., Giarlo, G., Ricciutelli, M., Ballini, R., Georg, G. I., VanderVelde, D. G., Himes, R. H., Wang, M., Lakdawala, A., Snyder, J. P. |
| Zdroj: |
Organic Letters; February 2004, Vol. 6 Issue: 4 p461-464, 4p |
| Abstrakt: |
We have previously described a model of paclitaxel−microtubule binding that led to the prediction that analogues of paclitaxel lacking any D ring could stabilize microtubules as well as paclitaxel if the substituent present at C4 did not have unfavorable steric interactions with the binding pocket. We report the synthesis of a 4-methyl paclitaxel analogue, compound 1, which bears this prediction out. Compound 1 is as potent as paclitaxel at microtubule stabilization in vitro; however, it has only about one-four-hundredth the cytotoxicity of paclitaxel. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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