American Chemical Society
ol1000473_si_001.pdf (2.34 MB)

“Clicktophycin-52”: A Bioactive Cryptophycin-52 Triazole Analogue

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journal contribution
posted on 2010-03-05, 00:00 authored by Markus Nahrwold, Tobias Bogner, Stefan Eissler, Spart Verma, Norbert Sewald
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.