新型氨基取代苯并噻吩并异吲哚啉的设计、合成及抗增殖活性。
Design, synthesis and antiproliferative activity of novel aminosubstituted benzothiopyranoisoindoles.
机构信息
Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):3110-2. doi: 10.1016/j.bmcl.2011.03.021. Epub 2011 Mar 11.
The synthesis of a number of new benzothiopyrano[4,3,2-cd]isoindole aminoderivatives designed as structural analogues of the key metabolite of the anticancer agent Ledacrine (nitracrine) and their in vitro cytotoxic activity evaluation against HCT-116, MES-SA, and MES-SA/Dx cancer cell lines is reported. The majority of the derivatives possessed noticeable cytotoxicity in a low μM range indicating an interesting structure-activity relationship.
报告了一系列新型苯并噻吩并[4,3,2-cd]异吲哚氨基衍生物的合成，这些衍生物被设计为抗癌药物拉司太嗪（硝拉西坦）的关键代谢物的结构类似物，并对 HCT-116、MES-SA 和 MES-SA/Dx 癌细胞系进行了体外细胞毒性活性评价。大多数衍生物在低 μM 范围内具有显著的细胞毒性，表明存在有趣的结构-活性关系。
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