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  1. Designed Epothilones: Combinatorial Synthesis, Tubulin Assembly Properties, abd Cytotoxic Action against Taxol-Resistant Tumor Cells
    K. C. Nicolaou, D. Vourloumis, T. Li, J. Pastor, N. Winssinger, Y. He, S. Ninkovic, F. Sarabia, H. Vallberg, F. Roschangar, N. P. King, M. R. V. Finlay, P. Giannakakou, P. Verdier-Pinard, E. Hamel
    Angew. Chem. Int. Ed. Engl. 1997, 36, 2097-2103

A library of epothilone A and B analogues, which was constructed by solid-phase combinatorial synthesis using SMART Microreactors and solution chemistry, was screened in two different tubulin binding assays. Selected compounds were subjected to cytotoxicity studies against a number of cell lines, including Taxol-resistant cells. Important structure-activity relationship emerged from these studies, which sets the stage for further discoveries and developments in the anticancer field.

DOI: 10.1002/anie.199720971 

open archive unige:24442