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Herein we report structure-cytotoxicity relationships for analogues of N-desacetoxytubulyisn H 1. A novel synthetic approach toward 1 enabled the discovery of compounds with a range of activity. Calculated basicity of the N-terminus of tubulysins was shown to be a good predictor of cytotoxicity. The impact of structural modifications at the C-terminus of 1 upon cytotoxicity is also described. These findings will facilitate the development of new tubulysin analogues for the treatment of cancer.
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| http://dx.doi.org/10.1021/acs.jmedchem.6b01023 | DOI Listing |
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