一些 6H-吲哚并[2,3-b]喹喔啉的合成、抗癌和细胞抑制活性。
Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b]quinoxalines.
机构信息
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560010, India.
出版信息
Acta Pharm. 2009 Dec;59(4):431-40. doi: 10.2478/v10007-009-0040-9.
Various 6-aralkyl-9-substituted-6H-indolo[2,3-b]quinoxalines were synthesized by reaction of 1,5-disubstituted 2,3-dioxo-2,3-dihydroindole and orthophenylene diamine. Appreciable anticancer activity of compounds 5b, 5d, 5g and 5l at various cell lines among 59 human tumor cell panels was observed. All the synthesized compounds were evaluated for cytostatic activity against human Molt 4/C8 and CEM T-lymphocytes as well as for murine L1210 leukemia cells. Compound 5h exhibited an I C50 of 23 micromol L(-1) against Molt 4/C8 and 38 micromol L(-1) against CEM compared to melphalan 3.2 micromol L(-1) and 2.5 micromol L(-1), respectively. The IC(50) for compound 7i against L1210 was 7.2 micromol L(-1) compared to melphalan 2.1 micromol L(-1).
多种 6-芳基-9-取代-6H-吲哚并[2,3-b]喹喔啉通过 1,5-二取代 2,3-二氧代-2,3-二氢吲哚与邻苯二胺反应合成。在 59 个人类肿瘤细胞系中，化合物 5b、5d、5g 和 5l 在各种细胞系中表现出显著的抗癌活性。所有合成的化合物都针对人 Molt 4/C8 和 CEM T 淋巴细胞以及鼠 L1210 白血病细胞进行了细胞抑制活性评估。化合物 5h 对 Molt 4/C8 的 IC50 为 23 微摩尔/升，对 CEM 的 IC50 为 38 微摩尔/升，而美法仑的 IC50 分别为 3.2 微摩尔/升和 2.5 微摩尔/升。化合物 7i 对 L1210 的 IC50 为 7.2 微摩尔/升，而美法仑的 IC50 为 2.1 微摩尔/升。
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