期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 1, 页码 134-142出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801064y
关键词
-
资金
- ANR [ANR-05-BLAN-0292]
- Agence Nationale de la Recherche (ANR) [ANR-05-BLAN-0292] Funding Source: Agence Nationale de la Recherche (ANR)
Ten hybrids of vinca alkaloids and phomopsin A have been synthesized by linking the octahydrophomopsin lateral chain to the tertiary amine of the cleavamine moiety of anhydrovinblastine (AVLB) and vinorelbine. These compounds have been elaborated in order to obtain original products that may interfere with both binding sites of vinblastine (VLB) and phomopsin in tubulin. Although NMR and molecular modeling studies have shown that the orientation of the added peptide chains of these hybrids is not the same as those of phomopsin A, most of them are very potent inhibitors of microtubules assembly and they present good cytotoxicity against KB cell line. These interesting biological activities may eventually be explained by the fact that their lateral chain resides in a pocket distinct from that of the phomopsin A peptide, at the interface of tubulins beta and alpha.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据