Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs.

Padron JM; Miranda PO; Padron JI; Martin VS

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Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs.

机译：β'-羟基-α，β-不饱和酮：用于设计抗癌药物的新药效基团。

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A series of beta'-hydroxy-alpha,beta-unsaturated ketones were prepared by means of an iron(III) catalyzed domino process. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, SW1573, and WiDr. The results showed that beta'-hydroxy-alpha,beta-unsaturated ketones were more potent than alpha,beta-unsaturated ketones. The best activity profiles were obtained for the derivatives bearing cyclic or branched substituents on the side chains.

机译：借助于铁（III）催化的多米诺法制备了一系列β'-羟基-α，β-不饱和酮。在人实体瘤细胞系A2780，SW1573和WiDr中检查了体外抗增殖活性。结果表明，β'-羟基-α，β-不饱和酮比α，β-不饱和酮更有效。对于在侧链上带有环状或支链取代基的衍生物，获得了最佳的活性曲线。

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《Bioorganic and Medicinal Chemistry Letters》 |2006年第8期|共4页
作者
Padron JM; Miranda PO; Padron JI; Martin VS;
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正文语种 eng
中图分类药学;生物化学;
关键词
Antineoplastic Agents; Cell Proliferation; Iron; Ketones; 抗肿瘤药; 铁; 酮类;

机译：Antineoplastic Agents;Cell Proliferation;Iron;Ketones;抗肿瘤药;铁;酮类;

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1. Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs. [J] . Padron JM, Miranda PO, Padron JI, Bioorganic and Medicinal Chemistry Letters . 2006,第8期

机译：β'-羟基-α，β-不饱和酮：用于设计抗癌药物的新药效基团。
2. Multiple QSAR models, pharmacophore pattern and molecular docking analysis for anticancer activity of alpha, beta-unsaturated carbonyl-based compounds, oxime and oxime ether analogues [J] . Masand Vijay H., El-Sayed Nahed N. E., Bambole Mukesh U., Journal of Molecular Structure . 2018,第期

机译：α，β-不饱和羰基化合物，肟和肟醚类似物的抗癌活性的多种QSAR模型，药物图案和分子对接分析
3. Structure-activity relationships of novel dithiocarbamates containing alpha,beta-unsaturated ketone fragment as potent anticancer agents [J] . Wang Yuanqiang, Li Ridong, Zhang Han, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2019,第7期

机译：含有α，β不饱和酮片段的新型二硫代氨基酯作为有效抗癌剂的结构 - 活性关系
4. Catalytic 1,4-Reduction of alpha,beta-Unsaturated Ketones and Application to Asymmetric Synthesis of Warfarin [C] . Yasunori Tsuchiya, Ken-ichi Moriya, Christine Beemelmanns Symposium on Organometallic Chemistry . 2006

机译：催化1,4-减少α，β-不饱和酮和施用于Warfarin的不对称合成
5. Molecular Design for a Novel Organotin Hydride and Ferric Chloride Mediated Michael Addition of Dicarboxylic Acid Esters to alpha,beta-Unsaturated Ketones. [D] . Deka, Dibakar Chandra. 2010

机译：新型有机锡氢化物和氯化铁介导的二羧酸酯向α，β-不饱和酮的迈克尔加成反应的分子设计。
6. Structure-Based Pharmacophore Design and Virtual Screening for Novel Tubulin Inhibitors with Potential Anticancer Activity [O] . Yunjiang Zhou, Bin Di, Miao-Miao Niu 2019

机译：具有潜在抗癌活性的新型微管蛋白抑制剂的基于结构的药理学设计和虚拟筛选
7. Conjugate Addition of Lithium Dimethylcuprate to an alpha,beta,beta,-Trialkylthio-alpha,beta-unsaturated Ketone. [O] . Øyvind Hammer Johansen, Kjell Undheim, Margareta Curvall, 1979

机译：将二甲基丙酸锂的缀合物加入α，β，β， - 三酮烷基硫酮，β-不饱和酮。

Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs.

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