Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides
Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides
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DOI：
10.1021/ol007049u
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发表时间：
2001-04-05
期刊：
影响因子：
5.2
通讯作者：
Pisano, C
中科院分区：
文献类型：
--
作者：
Belvisi, L;Bernardi, A;Pisano, C
为了开发具有活性和选择性的整合素拮抗剂，合成了一个含有6，5-和7，5-稠环内酰胺类立体异构体的环状RGD假五肽文库。描述了这些RGD衍生物的固相合成和活性，该方法导致了两个已知的最活跃的α(V)β(3)受体抑制剂。
A small library of cyclic RGD pseudopentapeptides incorporating stereoisomeric 6,5- and 7,5-fused bicyclic lactams was synthesized with the aim of developing active and selective integrin antagonists. The solid-phase synthesis and activity of these RGD derivatives is described, The approach led to two of the most active known inhibitors of alpha (v)beta (3) receptor.