| Literature DB >> 27809515 |
Dorin Toader1,2, Fengjiang Wang1, Lakshmaiah Gingipalli1, Melissa Vasbinder1, Mark Roth1, Shenlan Mao3, Michael Block1, Jay Harper3, Sambaiah Thota1, Mei Su1, Jianquo Ma1, Vahe Bedian1, Adeela Kamal3.
Abstract
Herein we report structure-cytotoxicity relationships for analogues of N14-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.Entities:
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Year: 2016 PMID： 27809515 DOI： 10.1021/acs.jmedchem.6b01023
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446