7H-苯并[7,8]色烯并[2,3-d]嘧啶-8-胺的简便合成及其抗增殖活性
Facile synthesis and antiproliferative activity of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines.
作者信息
Akrami Hamidreza, Safavi Maliheh, Mirjalili Bibi Fatemeh, Dehghani Ashkezari Mahmood, Dadfar Farhang, Mohaghegh Najme, Emami Saeed, Salehi Fahimeh, Nadri Hamid, Ardestani Sussan K, Firoozpour Loghman, Khoobi Mehdi, Foroumadi Alireza
机构信息
Department of Chemistry, College of Science, Yazd University, Yazd, PO Box 8915813149, Iran.
Department of Biotechnology, Iranian Research Organization for Science and Technology (IROST), Tehran, Iran.
出版信息
Eur J Med Chem. 2017 Feb 15;127:128-136. doi: 10.1016/j.ejmech.2016.12.037. Epub 2016 Dec 21.
A series of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines 6a-t were synthesized as new potential antiproliferative agents. The in vitro antiproliferative activity evaluation of title compounds using MTT assay revealed that most compounds showed significant activity against tested cancer cell lines (A549, MOLT-4, and HeLa). The 2-fluoro-aniline derivatives 6e and 6l were the most active compounds against A549 and MOLT-4 cells, respectively. The benzylamine analog 6h showed superior activity against HeLa cells. However, compound 6l with IC values of 5.2-6.9 μM had the best profile of activity against all tested cell lines. The morphological and flow cytometric analyses showed that compound 6l can induce apoptosis in the MOLT-4 cells.
合成了一系列7H-苯并[7,8]色烯并[2,3-d]嘧啶-8-胺6a-t作为新型潜在的抗增殖剂。使用MTT法对标题化合物进行体外抗增殖活性评估，结果表明大多数化合物对测试的癌细胞系（A549、MOLT-4和HeLa）显示出显著活性。2-氟苯胺衍生物6e和6l分别是对A549和MOLT-4细胞活性最高的化合物。苄胺类似物6h对HeLa细胞表现出优异的活性。然而，IC值为5.2-6.9 μM的化合物6l对所有测试细胞系具有最佳的活性概况。形态学和流式细胞术分析表明，化合物6l可诱导MOLT-4细胞凋亡。
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