Regioselective synthesis and initial evaluation of a folate receptor targeted rhaponticin prodrug

Regioselective synthesis and initial evaluation of a folate receptor targeted rhaponticin prodrug
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叶酸受体靶向土大黄素前药的区域选择性合成和初步评价

DOI:
10.1016/j.cclet.2012.08.006
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发表时间:
2012-10
期刊:
Chinese Chemieal Letters
影响因子:
--
通讯作者:
Fan Jun
Fan Jun
中科院分区:
其他
文献类型:
--
作者:
Liang Xu Hua;Sun Yang;Liu Lu Sha;Zhao Ying Yong;Hu Xiao Yun;Fan Jun

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为了提高土大黄素(Rhaponticin,RHA)的治疗效果,设计并区域选择性合成了一种以叶酸受体(FR)为靶点的RHA前体药物。并进行了一系列的体内外生物学评价。生物学研究的积极结果保证进一步的临床前研究之前,这种新的靶向化疗药物被认为是临床研究。
To improve the therapeutic effect of rhaponticin (RHA), a folate receptor (FR) targeted RHA prodrug was designed and regioselectively synthesized by utilizing a hydrophilic peptide spacer linked to folic acid (FA) via a releasable disulfide linker. A series of biological evaluation was investigated in vitro and in vivo. The positive results of biological investigations warrant further preclinical study before this novel targeted chemotherapeutic is considered for clinical investigation.
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