Synthesis and Antiproliferative Activity of Silybin Conjugates with Salinomycin and Monensin

Synthesis and Antiproliferative Activity of Silybin Conjugates with Salinomycin and Monensin
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DOI:
10.1111/cbdd.12602
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发表时间:
2015-12-01
影响因子:
3
通讯作者:
Huczynski, Adam
Huczynski, Adam
中科院分区:
医学4区
文献类型:
--
作者:
Antoszczak, Michal;Klejborowska, Greta;Huczynski, Adam

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为开发多靶点抗癌药物,在温和的酯化条件下,合成了新型水飞蓟宾(Silybin)与盐霉素(SAL)和莫能菌素(MON)的偶联物,并对其抗增殖活性进行了研究。所得结合物对肝癌细胞株HepG2、LoVo和LoVo/DX具有一定的抗癌活性。此外,MON-SIL结合物比相应的SAL-SIL结合物表现出更高的抗癌潜力和更好的选择性。
Aiming at development of multitarget drugs for the anticancer treatment, new silybin (SIL) conjugates with salinomycin (SAL) and monensin (MON) were synthesized, in mild esterification conditions, and their antiproliferative activity was studied. The conjugates obtained exhibit anticancer activity against HepG2, LoVo and LoVo/DX cancer cell lines. Moreover, MON-SIL conjugate exhibits higher anticancer potential and better selectivity than the corresponding SAL-SIL conjugate.