Isatin derivatives with activity against apoptosis-resistant cancer cells.
Isatin derivatives with activity against apoptosis-resistant cancer cells.
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DOI：
10.1016/j.bmcl.2016.02.015
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发表时间：
2016-03-15
影响因子：
2.7
通讯作者：
Kornienko A
中科院分区：
文献类型：
--
作者：
Evdokimov NM;Magedov IV;McBrayer D;Kornienko A
在对抗凋亡的癌细胞具有活性的小分子的研究中，合成了一系列基于靛红的杂环化合物，并发现其抑制抗凋亡的癌细胞系的增殖。这些化合物的合成涉及市售的活性亚甲基杂环与靛红的缩合，以中等至优异的产率进行。在目前的研究中制备的杂环支架似乎是开发具有细胞凋亡抗性的抗癌药物的有用起点，因此与令人沮丧的癌症有关。
In a search of small molecules active against apoptosis-resistant cancer cells, a series of isatin-based heterocyclic compounds were synthesized and found to inhibit proliferation of cancer cell lines resistant to apoptosis. The synthesis of these compounds involved a condensation of commercially available, active methylene heterocycles with isatin proceeding in moderate to excellent yields. The heterocyclic scaffolds prepared in the current investigation appear to be a useful starting point for the development of agents to fight cancers with apoptosis resistance, and thus, associated with dismal prognoses.