Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.

Shiina I; Sano Y; Nakata K; Kikuchi T; Sasaki A; Ikekita M; Hasome Y

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Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.

机译：新的伪对称他莫昔芬衍生物的合成及其抗肿瘤活性。

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Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-60 human acute promyelocytic leukemia, whereas 16 possesses medium activity against the cell line and 17 has no effect on the cell viability. The agarose gel electrophoresis for DNA cleavage showed the cell death might be induced by apoptosis.

机译：通过新型三组分偶联反应合成了三种新的拟对称他莫昔芬衍生物RID-B（15），C（16）和D（17），以及拟对称他莫昔芬衍生物的构效关系被检查了。已发现15强烈抑制HL-60人急性早幼粒细胞白血病的生存力，而16对细胞系具有中等活性，而17对细胞生存力没有影响。用于DNA切割的琼脂糖凝胶电泳显示细胞死亡可能是由凋亡诱导的。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2007年第9期|共4页
作者
Shiina I; Sano Y; Nakata K; Kikuchi T; Sasaki A; Ikekita M; Hasome Y;
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正文语种 eng
中图分类药学;生物化学;
关键词
derivatives; Tamoxifen; Synthesis; Neoplasms; novel; 他莫昔芬; 肿瘤;

机译：derivatives;Tamoxifen;Synthesis;Neoplasms;novel;他莫昔芬;肿瘤;

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1. Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity. [J] . Shiina I, Sano Y, Nakata K, Bioorganic and Medicinal Chemistry Letters . 2007,第9期

机译：新的伪对称他莫昔芬衍生物的合成及其抗肿瘤活性。
2. Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents. [J] . Shiina I, Sano Y, Nakata K, Biochemical Pharmacology . 2008,第5期

机译：新型拟对称他莫昔芬衍生物作为抗肿瘤剂的合成及药理评价。
3. Synthesis, chiral resolution, and determination of novel furan lignan derivatives with potent anti-tumor activity. [J] . Sun HL, Wang TT, Lv ZL, Bioorganic and Medicinal Chemistry Letters . 2010,第6期

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5. TNF-related apoptosis-inducing ligand (TRAIL/Apo-2L): A novel mechanism for CpG ODN and BCG-induced anti-tumor activity. [D] . Kemp, Troy Jon. 2005

机译：TNF相关凋亡诱导配体（TRAIL / Apo-2L）：CpG ODN和BCG诱导的抗肿瘤活性的新机制。
6. Uses of Cyanoacetylhydrazine in Heterocyclic Synthesis: Novel Synthesis of Pyrazole Derivatives with Anti-tumor Activities [O] . Rafat M. Mohareb, Nahed N. E. El-Sayed, Mahmoud A. Abdelaziz 2012

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Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.

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