Anticancer Ru-II and Rh-III Piano-Stool Complexes that are Histone Deacetylase Inhibitors

Cross Jasmine M.; Blower Tim R.; Gallagher Natalie; Gill Jason H.; Rockley Kimberly L.; Walton James W.

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Anticancer Ru-II and Rh-III Piano-Stool Complexes that are Histone Deacetylase Inhibitors

机译：抗癌Ru-II和RH-III钢琴堆综合体是组蛋白脱乙酰酶抑制剂

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The first examples of Ru-II and Rh-III piano-stool complex histone deacetylase (HDAC) inhibitors are presented. The novel complexes have antiproliferative activity against H460 non-small-cell lung carcinoma cells that is comparable to the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (SAHA). Strong evidence for HDAC inhibition as a primary mechanism of action is provided. The complexes reported here represent an important step towards the design of highly active and selective HDAC inhibitors.

机译：提出了Ru-II和RH-III钢琴型络合物组蛋白脱乙酰酶（HDAC）抑制剂的第一个实例。该新型配合物具有针对H460非小细胞肺癌细胞的抗增殖活性，其与临床使用的HDAC抑制剂Suberoylanilide羟肟酸（Saha）相当。提供了作为主要行动机制的HDAC抑制的强大证据。这里报道的复合物代表了朝向高活性和选择性HDAC抑制剂设计的重要一步。

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来源
《ChemPlusChem》 |2016年第12期|共5页
作者
Cross Jasmine M.; Blower Tim R.; Gallagher Natalie; Gill Jason H.; Rockley Kimberly L.; Walton James W.;
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作者单位

Univ Durham Dept Chem South Rd Durham DH1 3LE England;

Univ Durham Sch Biol &

Biomed Sci South Rd Durham DH1 3LE England;

Univ Durham Wolfson Res Inst Sch Med Pharm &

Hlth Queens Campus Stockton On Tees TS17 6BH;

Univ Durham Wolfson Res Inst Sch Med Pharm &

Hlth Queens Campus Stockton On Tees TS17 6BH;

Univ Durham Wolfson Res Inst Sch Med Pharm &

Hlth Queens Campus Stockton On Tees TS17 6BH;

Univ Durham Dept Chem South Rd Durham DH1 3LE England;

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原文格式 PDF
正文语种 eng
中图分类化学;
关键词
antitumour agents; bioorganometallic chemistry; histone deacetylase inhibitors; piano-stool complexes; ruthenium;

机译：抗肿瘤剂;生物管状物化化学;组蛋白脱乙酰酶抑制剂;钢琴凳;钌;

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1. Anticancer Ru-II and Rh-III Piano-Stool Complexes that are Histone Deacetylase Inhibitors [J] . Cross Jasmine M., Blower Tim R., Gallagher Natalie, ChemPlusChem . 2016,第12期

机译：抗癌Ru-II和RH-III钢琴堆综合体是组蛋白脱乙酰酶抑制剂
2. The histone deacetylase inhibitor butyroyloxymethyl diethylphosphate (AN-7) protects normal cells against toxicity of anticancer agents while augmenting their anticancer activity [J] . Nataly Tarasenko, Gania Kessler-Icekson, Pnina Boer, Investigational New Drugs . 2012,第1期

机译：组蛋白脱乙酰基酶抑制剂丁酰氧基甲基二乙基磷酸酯（AN-7）保护正常细胞抵抗抗癌药的毒性，同时增强其抗癌活性
3. The histone deacetylase inhibitor butyroyloxymethyl diethylphosphate (AN-7) protects normal cells against toxicity of anticancer agents while augmenting their anticancer activity [J] . TarasenkoN., Kessler-IceksonG., BoerP., Investigational new drugs. . 2012,第1期

机译：组蛋白脱乙酰基酶抑制剂丁酰氧基甲基二乙基磷酸酯（AN-7）保护正常细胞免受抗癌药的毒性，同时增强其抗癌活性
4. The Tricyclic Antidepressant Amitriptyline Inhibits D-Cyclin Transactivation and Induces Myeloma Cell Apoptosis by Inhibiting Histone Deacetylases: In Vitro and In Silico Evidence [C] . Xinliang Mao, Depei Wu, Suzanne Trudel, International conference of molecular simulations and applied informatics technologies . 2012

机译：三环抗抑郁药阿米替林通过抑制组蛋白脱乙酰基酶抑制D-cyclin反式激活并诱导骨髓瘤细胞凋亡：体外和计算机证据。
5. Anti-ovarian cancer effects of histone deacetylase inhibitors and calpain inhibitor. [D] . Lapinska, Karolina Eva. 2016

机译：组蛋白脱乙酰基酶抑制剂和钙蛋白酶抑制剂的抗卵巢癌作用。
6. Chromium Cross-Links Histone Deacetylase 1-DNA Methyltransferase 1 Complexes to Chromatin, Inhibiting Histone-Remodeling Marks Critical for Transcriptional Activation [O] . Michael Schnekenburger, Glenn Talaska, Alvaro Puga 2006

机译：铬交联组蛋白去乙酰化酶1-DNA甲基转移酶1络合物对染色质，抑制组蛋白重塑标记对于转录激活至关重要。
7. Anticancer RuII and RhIII piano-stool complexes that are histone deacetylase inhibitors. [O] . Cross J.M., Blower T.R., Gallagher N., 2016

机译：作为组蛋白脱乙酰基酶抑制剂的抗癌RuII和RhIII钢琴凳复合物。

Anticancer Ru-II and Rh-III Piano-Stool Complexes that are Histone Deacetylase Inhibitors

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