Synthesis of (3R)-amino-(2S)-hydroxy amino acids for inhibition of methionine aminopeptidase-1

被引:29
作者
Keding, SJ
Dales, NA
Lim, SJ
Beaulieu, D
Rich, DH
机构
[1] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA
[2] Univ Wisconsin, Sch Pharm, Madison, WI 53706 USA
[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
基金
美国国家卫生研究院;
关键词
D O I
10.1080/00397919808004481
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
(3R)-amino-(2S)-hydroxy heptanoic acid (AHHpA) was synthesized via asymmetric aminohydroxylation and coupled with di- and tripeptides to form three compounds that inhibit MetAP-1 with IC50 values in the low micromolar range.
引用
收藏
页码:4463 / 4470
页数:8
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