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Total synthesis and biological evaluation of nannocystin analogues modified at the polyketide phenyl moiety
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2018-07-10 , DOI: 10.1016/j.tetlet.2018.07.028
Yunfeng Tian , Yahui Ding , Xiaolong Xu , Yanju Bai , Yang Tang , Xin Hao , Weicheng Zhang , Yue Chen

Total synthesis of a focused set of 10 nannocystin analogues 3a3j modified at the polyketide phenyl moiety was reported. These compounds were evaluated against three cancer cell lines. Compared with the naturally occurring congener 3a, the other synthetic variants either preserved or lose antiproliferative activity at varying degrees. Moreover, the potent analogues also displayed comparable levels of cytotoxicity toward two normal cell lines.



中文翻译:

聚酮化合物苯基部分修饰的nannocystin类似物的全合成和生物学评估

据报道,在聚酮化合物苯基部分修饰的一组集中的10种纳米囊藻毒素类似物3a3j的总合成。针对三种癌细胞系评估了这些化合物。与天然同源物3a相比,其他合成变体在不同程度上保留或丧失了抗增殖活性。而且,有效的类似物对两种正常细胞系也显示出可比较的细胞毒性水平。

更新日期:2018-07-10
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