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
|Titolo:||Synthesis, modeling, and anti-tubulin activity of a D-seco paclitaxel analogue|
|Autori interni:||BARBONI, Luciano|
|Data di pubblicazione:||2004|
|Appare nelle tipologie:||Articolo|
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