A new synthesis of 6-N-hydroxy-4-(2-methyl-l,2,3,4-tetrahydro-pyrido[4,3-b] indol-5-ylmethyl)benzamide, tubastatin a, a highly selective inhibitor of histone deacetylase

Kozlov M.V.; Kleymenova A.A.; Konduktorov K.A.; Kochetkov S.N.

首页> 外文期刊>Russian journal of bioorganic chemistry >A new synthesis of 6-N-hydroxy-4-(2-methyl-l,2,3,4-tetrahydro-pyrido[4,3-b] indol-5-ylmethyl)benzamide, tubastatin a, a highly selective inhibitor of histone deacetylase

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A new synthesis of 6-N-hydroxy-4-(2-methyl-l,2,3,4-tetrahydro-pyrido[4,3-b] indol-5-ylmethyl)benzamide, tubastatin a, a highly selective inhibitor of histone deacetylase

机译：一种6-N-羟基-4-（2-甲基-1,2,3,4-四氢-吡啶并[4,3-b]吲哚-5-基甲基）苯甲酰胺的新合成物，tubastatin a，一种高度选择性的抑制剂蛋白脱乙酰基酶

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摘要

A highly selective inhibitor of histone deacetylase 6, tubastatin A, was synthesized in four steps under smooth and safe reaction conditions.

机译：在平稳，安全的反应条件下，通过四个步骤合成了高度选择性的组蛋白脱乙酰基酶6（抗坏血酸抑素A）抑制剂。

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《Russian journal of bioorganic chemistry》 |2013年第1期|共4页
作者
Kozlov M.V.; Kleymenova A.A.; Konduktorov K.A.; Kochetkov S.N.;
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正文语种 eng
中图分类生物化学;
关键词
histone deacetylase 6; hydroxamic acids; indoles;

机译：组蛋白脱乙酰基酶6;异羟肟酸;吲哚;

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1. A new synthesis of 6-N-hydroxy-4-(2-methyl-l,2,3,4-tetrahydro-pyrido[4,3-b] indol-5-ylmethyl)benzamide, tubastatin a, a highly selective inhibitor of histone deacetylase [J] . Kozlov M.V., Kleymenova A.A., Konduktorov K.A., Russian journal of bioorganic chemistry . 2013,第1期

机译：一种6-N-羟基-4-（2-甲基-1,2,3,4-四氢-吡啶并[4,3-b]吲哚-5-基甲基）苯甲酰胺的新合成物，tubastatin a，一种高度选择性的抑制剂蛋白脱乙酰基酶
2. Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects [J] . VishwakarmaS., IyerL.R., MuleyM., International immunopharmacology . 2013,第1期

机译：Tubastatin是一种选择性的组蛋白脱乙酰基酶6抑制剂，具有抗炎和抗风湿作用
3. Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl) propylamino]-8-methyl-8 H -pyrido[2,3- d ]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2 H -pyran-4-ylamino)pyrido[2,3- d ]pyrimidin-7(8 H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase [J] . Goldstein D.M., Soth M., Gabriel T., Journal of Medicinal Chemistry . 2011,第7期

机译：6-（2,4-二氟苯氧基）-2- [3-羟基-1-（2-羟乙基）丙基氨基] -8-甲基-8 H-吡啶基[2,3-d]嘧啶-7-one（ pamapimod）和6-（2,4-二氟苯氧基）-8-甲基-2-（四氢2 H-吡喃-4-基氨基）吡啶并[2,3-d]嘧啶7（8 H）-一（R1487 ）作为p38α丝裂原活化蛋白激酶的口服生物利用度和高选择性抑制剂
4. A bridge between natural products to cancer drugs:Toward subclass selective cyclic-peptide-inhibitors of histone deacetylases [C] . Norikazu Nishino, Binoy Jose, Tamaki Kato International Peptide Symposium;European Peptide Symposium . 2005

机译：天然产物与癌症药物之间的桥梁：朝向组蛋白脱乙酰酶的亚类选择性环肽抑制剂
5. The structural requirements of histone deacetylase (HDAC) inhibitors: Suberoylanilide hydroxamic acid (SAHA) analogues modified at C3, C6, and C7 positions enhance selectivity [D] . Choi, Sun Ea 2012

机译：组蛋白脱乙酰基酶（HDAC）抑制剂的结构要求：在C3，C6和C7位置修饰的Suberoylanilide异羟肟酸（SAHA）类似物可提高选择性
6. From the Cover: The benzamide MS-275 is a potent long-lasting brain region-selective inhibitor of histone deacetylases [O] . M. V. Simonini, L. M. Camargo, E. Dong, 2006

机译：从封面开始：苯甲酰胺MS-275是一种有效持久的组蛋白脱乙酰基酶脑区域选择性抑制剂
7. Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor [O] . -1

机译：Timastatin A的结构和体内表征，一种广泛使用的组蛋白脱乙酰酶6抑制剂

A new synthesis of 6-N-hydroxy-4-(2-methyl-l,2,3,4-tetrahydro-pyrido[4,3-b] indol-5-ylmethyl)benzamide, tubastatin a, a highly selective inhibitor of histone deacetylase

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