A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4.

Bega Luis A S; Beatriz Adilson; Sarkar Taradas; Hamel Ernest; do Amaral Marcos S; de Lima Dênis Pires

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A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4.

机译：二芳基硫醚，亚砜和砜与康维他汀A-4的结构相似。

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Studies examining various spacer groups that link the two aromatic rings of combretastatin A-4 (CA4) have shown that the biological activity of analogs does not require the cis-stilbene configuration of CA4. Oxygen or nitrogen, carbonyl, methylene and ethylene spacers, for example, are present in CA4 analogs that show good activity. Up to now sulfur was not tested for this purpose. In this article we describe the synthesis of sulfide, sulfoxide and sulfone spacers between two aromatic rings comparable to those of CA4. We also compared them with CA4 for inhibitory effects on cell growth, tubulin polymerization, and the binding of [(3)H]colchicine to tubulin. We found that the sulfide is highly active and may be a lead compound for the preparation of antitumor compounds.

机译：研究检查了连接康维他汀A-4（CA4）两个芳香环的各种间隔基的研究表明，类似物的生物活性不需要CA4的顺-二苯乙烯构型。例如，氧或氮，羰基，亚甲基和乙烯间隔基存在于显示出良好活性的CA4类似物中。到目前为止，尚未为此目的测试硫。在本文中，我们描述了可与CA4相比的两个芳环之间的硫化物，亚砜和砜间隔基的合成。我们还比较了它们与CA4对细胞生长，微管蛋白聚合以及[（3H）]秋水仙碱与微管蛋白的结合的抑制作用。我们发现硫化物具有很高的活性，可能是制备抗肿瘤化合物的先导化合物。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第6期|共4页
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Bega Luis A S; Beatriz Adilson; Sarkar Taradas; Hamel Ernest; do Amaral Marcos S; de Lima Dênis Pires;
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1. A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4. [J] . Bega Luis A S, Beatriz Adilson, Sarkar Taradas, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第6期

机译：二芳基硫醚，亚砜和砜与康维他汀A-4的结构相似。
2. Visible-Light-Driven Silver-Catalyzed One-Pot Approach: A Selective Synthesis of Diaryl Sulfoxides and Diaryl Sulfones [J] . Dong Hyuk Kim, Juyoung Lee, Anna Lee Organic letters . 2018,第3期

机译：可见光驱动的银催化的单罐方法：双亚芳基磺氧化物和二芳基砜的选择性合成
3. Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4. [J] . Hall JJ, Sriram M, Strecker TE, Bioorganic and Medicinal Chemistry Letters . 2008,第18期

机译：康布雷他汀A-4含氮三氟结构修饰的设计，合成，生化和生物学评估。
4. Diallylammonium salts containing nitrogen, ethyl ester and sulfide, sulfoxide or sulfone motifs of amino acid residues of methionine polymer as green corrosion inhibitors [C] . Mohammad A. Jafar Mazumder, Lipiar K. M., Osman Goni, European corrosion congress;International corrosion congress;Pprocess safety congress . 2017

机译：甲硫氨酸聚合物氨基酸残基的氮，乙酯和硫化物，亚砜或砜基序的二烯丙基铵盐作为绿色缓蚀剂
5. Synthesis of 2-alkoxy-2-phenylpropionic acids; and nitrogen- and chlorine-containing derivatives of combretastatin A-4. [D] . Monk, Keith A. 2004

机译：2-烷氧基-2-苯基丙酸的合成；和康布雷他汀A-4的含氮和氯的衍生物。
6. A diaryl sulfide sulfoxide and sulfone bearing structural similarities to combretastatin A-4 [O] . Euzébio G. Barbosa, Luis A.S. Bega, Adilson Beatriz, -1

机译：与康维他汀A-4具有结构相似性的二芳基硫醚亚砜和砜
7. A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4 [O] . Euzébio G. Barbosa, Luis A.S. Bega, Adilson Beatriz, 2009

机译：硫化芳基，亚砜和砜轴承结构相同与梳子酸酯A-4
8. P-Chlorophenyl Methyl Sulfide, p-Chlorophenyl Methyl Sulfoxide, and p-Chlorophenyl Methyl Sulfone. 1. Acute Toxicity and Bacterial Mutagenicity Studies [R] . Leber, A. P., Dacre, J. C., Thake, D. C., 1993

机译：对氯苯基甲基硫醚，对氯苯基甲基亚砜和对氯苯基甲基砜。 1.急性毒性和细菌致突变性研究

A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4.

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