Synthesis and antitumor activity of selenium-containing quinone-based triazoles possessing two redox centres, and their mechanistic insights.
Synthesis and antitumor activity of selenium-containing quinone-based triazoles possessing two redox centres, and their mechanistic insights.
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DOI：
10.1016/j.ejmech.2016.06.019
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发表时间：
2016-10-21
影响因子：
6.7
通讯作者：
da Silva Junior, Eufranio N.
中科院分区：
文献类型：
--
作者：
da Cruz, Eduardo H. G.;Silvers, Molly A.;Jardim, Guilherme A. M.;Resende, Jarbas M.;Cavalcanti, Bruno C.;Bomfim, Igor S.;Pessoa, Claudia;de Simone, Carlos A.;Botteselle, Giancarlo V.;Braga, Antonio L.;Nair, Divya K.;Namboothiri, Irishi N. N.;Boothman, David A.;da Silva Junior, Eufranio N.
使用点击化学（铜催化的叠氮化物-炔1，3-偶极环加成）合成基于含硒醌的1，2，3-三唑，并针对六种类型的癌细胞系进行评价：HL-60（人早幼粒细胞白血病细胞），HCT-116（人结肠癌细胞）、PC 3（人前列腺细胞）、SF 295（人胶质母细胞瘤细胞）、MDA-MB-435（黑色素瘤细胞）和OVCAR-8（人卵巢癌细胞）。一些化合物显示IC 50值< 0.3 μM。还使用非肿瘤细胞，例如外周血单核细胞（PBMC）、V79和L929细胞，测定评价的醌类的细胞毒性潜力。还阐明了NAD（P）H：醌氧化还原酶1（NQO 1）的机制作用。这些化合物可以为更有效的抗癌药物开发和递送提供有前途的新的先导衍生物，并代表了已报道的最具活性的拉帕醌类之一。通过点击化学反应设计并合成了含硒醌类化合物，并对几种人癌细胞系进行了评价，在某些情况下，IC 50值低于0.3 μM。
Selenium-containing quinone-based 1,2,3-triazoles were synthesized using click chemistry, the copper catalyzed azide-alkyne 1,3-dipolar cycloaddition, and evaluated against six types of cancer cell lines: HL-60 (human promyelocytic leukemia cells), HCT-116 (human colon carcinoma cells), PC3 (human prostate cells), SF295 (human glioblastoma cells), MDA-MB-435 (melanoma cells) and OVCAR-8 (human ovarian carcinoma cells). Some compounds showed IC50 values < 0.3 μM. The cytotoxic potential of the quinones evaluated was also assayed using non-tumor cells, exemplified by peripheral blood mononuclear (PBMC), V79 and L929 cells. Mechanistic role for NAD(P)H:Quinone Oxidoreductase 1 (NQO1) was also elucidated. These compounds could provide promising new lead derivatives for more potent anticancer drug development and delivery, and represent one of the most active classes of lapachones reported. Selenium-containing quinones were designed and synthesized by click chemistry reaction and evaluated against several human cancer cell lines showing, in some cases, IC50 values below 0.3 μM.
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过氧化氢酶消除了NQO1阳性乳腺癌中的β-拉帕酮诱导的PARP1过度激活导向的坏死。
影响因子：
5.7
作者：
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影响因子：
3.5
作者：
da Cruz, Eduardo H. G.;Hussene, Caio M. B.;da Silva Junior, Eufranio N.
通讯作者：
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影响因子：
11.2
作者：
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通讯作者：
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DOI：
10.1073/pnas.90.15.7200
发表时间：
1993-08-01
影响因子：
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作者：
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影响因子：
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作者：
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通讯作者：
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