Self-assembling Releasable Thiocolchicine Diphenylbutenylaniline Conjugates
Self-assembling Releasable Thiocolchicine Diphenylbutenylaniline Conjugates
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DOI：
10.1021/acsmedchemlett.8b00605
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发表时间：
2019-04-01
影响因子：
4.2
通讯作者：
Passarella, Daniele
中科院分区：
文献类型：
--
作者：
Fumagalli, Gaia;Polito, Laura;Passarella, Daniele
报道了新型自组装共轭物的设计与合成。目标化合物的特征在于存在确保由脂肪酶裂解诱导的受控释放的自分解接头。以4-（1，2-二苯基丁-1-烯-1-基）苯胺为自组装诱导剂，氨基硫代秋水仙碱为原型药物。硫代秋水仙碱衍生物的释放已被证明在体外存在的猪胰脂肪酶和硅藻土支持的脂肪酶。通过动态光散射、原子力显微镜和荧光显微镜证实了纳米颗粒的形成。抗增殖活性已在两种人癌细胞系上得到证实。
The design and the synthesis of new self-assembling conjugates is reported. The target compounds are characterized by the presence of a self-immolative linker that secures a controlled release induced by lipase cleavage. 4-(1,2-Diphenylbut-1-en-1yl)aniline is used as a self-assembling inducer and aminothiocolchicine as prototype of drug. The release of thiocolchicine derivative has been demonstrated in vitro in the presence of porcine pancreatic lipase and Celite-supported lipase. The formation of nanoparticles is confirmed by dynamic light scattering, atomic force microscopy, and fluorescence microscopy. The antiproliferative activity has been proved on two human cancer cell lines.