Synthesis and biological evaluation of novel cryptophycin analogs with modification in the β-alanine region

被引:56
作者
Shih, C [1 ]
Gossett, LS
Gruber, JM
Grossman, CS
Andis, SL
Schultz, RM
Worzalla, JF
Corbett, TH
Metz, JT
机构
[1] Lilly Res Labs, Indianapolis, IN 46202 USA
[2] Wayne State Univ, Karmanos Canc Inst, Detroit, MI 48202 USA
关键词
D O I
10.1016/S0960-894X(98)00682-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Structure modification of the beta-alanine region (fragment C) of the potent antimitotic agent cryptophycin was investigated. This includes: (1) introduction of substituents at the previously unsubstituted C7 position of the macrolide ring and (:2) replacement of the (2R)-3-amino-2-methyl-propanoic acid (beta-alanine) with various (1)-amino acids to give the corresponding 15-membered unnatural cryptophycin analogs. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:69 / 74
页数:6
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