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  • Title: Synthesis and anticancer activity of novel quinoline-docetaxel analogues.
    Author: Chen M, Chen H, Ma J, Liu X, Zhang S.
    Journal: Bioorg Med Chem Lett; 2014 Jul 01; 24(13):2867-70. PubMed ID: 24835987.
    Abstract:
    A series of novel quinoline-docetaxel analogues (6a-6g, 13a-13g) were designed and synthesized by introducing bioactive quinoline scaffold to C2'-OH of docetaxel. The anticancer activities of these novel analogues were investigated against different human cancer cell lines including Hela, A549, A2780, MCF-7 and two resistant strains A2780-MDR and MCF-7-MDR. The data showed these analogues possessed similar to better cytotoxicity than docetaxel. Compound 6c was found to be the most potent one, and its IC50 value against MCF-7-MDR was 8.8 nM (IC50 of docetaxel was 180 nM). The work indicated that the introduction of quinolyl group in docetaxel could enhance cytotoxicity and reduce drug-resistance.
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