一些 6H-吲哚并[2,3-b]喹喔啉衍生物的设计、合成、细胞毒性评价和 QSAR 研究。
Design, synthesis, cytotoxic evaluation, and QSAR study of some 6H-indolo[2,3-b]quinoxaline derivatives.
机构信息
School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, India.
出版信息
J Enzyme Inhib Med Chem. 2010 Jun;25(3):394-405. doi: 10.3109/14756360903190747.
In the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure of the 6H-indolo[2,3-b]quinoxaline derivatives was confirmed by IR, NMR, Mass and elemental analysis. The compounds (IDQ-5, IDQ-10, IDQ-11, IDQ-13, and IDQ-14) exhibited significant in vitro activity against a human leukemia (HL-60) cell line. The QSAR derived for modeling the cytotoxic activity of 6H-indolo[2,3-b]quinoxaline derivatives suggests that candidate structures for increased cytotoxic potency should incorporate cyclic substituents or substituents with primary carbon atoms.
在抗癌药物开发的途径中，我们通过结构修饰设计并合成了一些 6H-吲哚并[2,3-b]喹喔啉衍生物（作为 DNA 嵌入剂）。6H-吲哚并[2,3-b]喹喔啉衍生物的结构通过 IR、NMR、Mass 和元素分析得到证实。这些化合物（IDQ-5、IDQ-10、IDQ-11、IDQ-13 和 IDQ-14）对人白血病（HL-60）细胞系表现出显著的体外活性。QSAR 用于建模 6H-吲哚并[2,3-b]喹喔啉衍生物的细胞毒性活性，表明候选结构应包含环状取代基或具有仲碳原子的取代基，以增加细胞毒性效力。
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