Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide
Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide
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DOI：
10.1016/j.bmcl.2006.07.030
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发表时间：
2006-10-01
影响因子：
2.7
通讯作者：
Leamon, Christopher P.
中科院分区：
文献类型：
--
作者：
Vlahov, Iontcho R.;Santhapuram, Hari Krishna R.;Leamon, Christopher P.
描述了叶酸受体（FR）靶向缀合物EC 145的有效合成。EC 145是维生素叶酸和强效细胞毒性剂脱乙酰长春碱单酰肼的水溶性衍生物。两个分子通过亲水性肽间隔子和还原不稳定的二硫键接头以区域选择性方式连接。(c)2006爱思唯尔有限公司版权所有。
An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described. EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, desacetylvinblastine monohydrazide. Both molecules are connected in regioselective manner via a hydrophilic peptide spacer and a reductively labile disulfide linker. (c) 2006 Elsevier Ltd. All rights reserved.