Synthesis and in vitro cytotoxic evaluation of aminoquinones structurally related to marine isoquinolinequinones.
Synthesis and in vitro cytotoxic evaluation of aminoquinones structurally related to marine isoquinolinequinones.
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合成和体外细胞毒性评估氨基酮与海洋等喹啉醌在结构上相关。
DOI：
10.3390/molecules17067042
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发表时间：
2012-06-07
期刊：
影响因子：
--
通讯作者：
Valderrama JA
中科院分区：
文献类型：
--
作者：
Delgado V;Ibacache A;Theoduloz C;Valderrama JA
报道了4-甲氧羰基-3-甲基异喹诺酮(1)及其取代产物的合成。用四甲基偶氮唑盐比色法测定了6，7和6，7取代的异喹诺酮类化合物的体外细胞毒活性。所有新合成的化合物对MRC-5健康肺成纤维细胞和四种人肿瘤细胞系：AGS胃腺癌、SK-MES-1肺癌、J82膀胱癌和HL-60白血病细胞均表现出中到高效的抑制作用。其中，化合物4b、12和13对人胃腺癌、人肺癌和人膀胱癌细胞具有良好的抗癌活性。7-氨基-6-溴异喹啉-5，8-醌(13)是最有希望的抗肿瘤活性化合物，其IC50值在0.21−0.49μM范围内，低于抗癌药物依托泊苷。
The synthesis of 4-methoxycarbonyl-3-methylisoquinolinequinone (1) and a variety of its substitution products with amino-, alkylamino and halogen groups on the quinone nucleus is reported. The series of 6-, 7- and 6,7-subtituted isoquinolinequinones were evaluated in vitro for their cytotoxic activity using the MTT colorimetric method. All the newly synthesized compounds showed moderate to high potency against MRC-5 healthy lung fibroblasts and four human tumor cell lines: AGS gastric adenocarcinoma, SK-MES-1 lung, J82 bladder carcinoma, and HL-60 leukemia cells. Among the series, compounds 4b, 12 and 13 exhibited interesting antitumor activity against human gastric adenocarcinoma, human lung and human bladder carcinoma cancer cells. 7-Amino-6-bromoisoquinoline-5,8-quinone (13) was found to be the most promising active compound against the tested cancer cell lines, with IC50 values in the 0.21−0.49 μM range, lower than the anti-cancer agent etoposide used as reference.
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影响因子：
1.8
作者：
Valderrama, Jaime A.;Andrea Ibacache, J.
通讯作者：
Andrea Ibacache, J.
影响因子：
1.8
作者：
Yoon, EY;Choi, HY;Kim, DJ
通讯作者：
Kim, DJ
DOI：
10.1007/s11101-009-9120-1
发表时间：
2009-06
期刊：
Phytochemistry reviews : proceedings of the Phytochemical Society of Europe
影响因子：
--
作者：
Nagle DG;Zhou YD
通讯作者：
Zhou YD
影响因子：
5.4
作者：
Gordaliza M
通讯作者：
Gordaliza M
影响因子：
5.4
作者：
Bhatnagar I;Kim SK
通讯作者：
Kim SK