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  • Title: "Clicktophycin-52": a bioactive cryptophycin-52 triazole analogue.
    Author: Nahrwold M, Bogner T, Eissler S, Verma S, Sewald N.
    Journal: Org Lett; 2010 Mar 05; 12(5):1064-7. PubMed ID: 20131817.
    Abstract:
    An endocyclic trans-amide linkage within the macrocyclic antitumor agent cryptophycin-52 was replaced by a 1,4-disubstituted 1H-1,2,3-triazole ring. Macrocyclisation of the triazole analogue was accomplished by macrolactamization as well as by Cu(I)-mediated "click"-cyclization. Compared to cryptophycin-52, in vitro cytotoxicity of "clicktophycin-52" against the multidrug resistant human cancer cell line KB-V1 is only slightly reduced.
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