“Clicktophycin-52”: a bioactive cryptophycin-52 triazole analogue

M Nahrwold, T Bogner, S Eissler, S Verma…

Index: Nahrwold, Markus; Bogner, Tobias; Eissler, Stefan; Verma, Spart; Sewald, Norbert Organic Letters, 2010 , vol. 12, # 5 p. 1064 - 1067

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Citation Number: 54

Abstract

An endocyclic trans-amide linkage within the macrocyclic antitumor agent cryptophycin-52 was replaced by a 1, 4-disubstituted 1 H-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.