1 research outputs found
Structure–Cytotoxicity Relationships of Analogues of <i>N</i><sup>14</sup>-Desacetoxytubulysin H
Herein
we report structure–cytotoxicity relationships for
analogues of <i>N</i><sup>14</sup>-desacetoxytubulyisn H <b>1</b>. A novel synthetic approach toward <b>1</b> enabled
the discovery of compounds with a range of activity. Calculated basicity
of the <i>N</i>-terminus of tubulysins was shown to be a
good predictor of cytotoxicity. The impact of structural modifications
at the C-terminus of <b>1</b> upon cytotoxicity is also described.
These findings will facilitate the development of new tubulysin analogues
for the treatment of cancer