"Clicktophycin-52": A Bioactive Cryptophycin-52 Triazole Analogue

被引：86

作者：

Nahrwold, Markus ^{[1
]}

Bogner, Tobias ^{[1
]}

Eissler, Stefan ^{[1
]}

Verma, Spart ^{[1
]}

Sewald, Norbert ^{[1
]}

机构：

[1] Univ Bielefeld, Dept Chem Organ & Bioorgan Chem, D-33615 Bielefeld, Germany

来源：

ORGANIC LETTERS | 2010年 / 12卷 / 05期

关键词：

CLICK CHEMISTRY; EFFICIENT SYNTHESIS; BIOLOGICAL EVALUATION; GROWING APPLICATIONS; SOLID-PHASE; PEPTIDE; 1,2,3-TRIAZOLE; DESIGN; CYCLOADDITIONS; INHIBITORS;

D O I：

10.1021/ol1000473

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：1064 / 1067

页数：4

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