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Synthesis, Evaluation and Molecular Modeling Study of L-2-amino-7/8-Bromoalkanoic Acid Derivatives as Histone Deacetylase Inhibitors

机译：L-2-氨基-7 / 8-溴烷酸衍生物作为组蛋白脱乙酰酶抑制剂的合成，评价和分子建模研究

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@@ Modulation of the acetylation state of lysine residues in the N-terminal of core histones plays a pivotal role in the regulation of gene expression[1,2]. Acetylation and deacetylation of histones are controlled by two corresponding enzymes, histone acetyltransferases (HATs) and histone deacetylases (HDACs)'31. In general, HDACs activity relates to transcriptional repression, and abnormal increase in HDACs activity has been associated with the development of some human cancers[4]. Studies indicated that inhibiting HDACs in tumor cells can induce growth arrest, cell proliferation and apoptosis. Therefore HDAC inhibitors (HDACIs) have become a promising class of anticancer agents[5]. Some natural and synthetic compounds have been reported as HDACIs. Almost all HDACIs are comprised of three parts: metal binding, linker and surface recognition domains[6].

机译：@@核心组末端赖氨酸残基的乙酰化状态在基因表达的调节中起枢转作用[1,2]。组蛋白的乙酰化和脱乙酰化由两种相应的酶，组蛋白乙酰转移酶（帽子）和组蛋白脱乙酰酶（HDACS）'31控制。通常，HDACs活性涉及转录抑制，HDACs活性的异常增加与一些人类癌症的发育有关[4]。研究表明，抑制肿瘤细胞中的HDAC可以诱导生长阻滞，细胞增殖和凋亡。因此，HDAC抑制剂（HDACIS）已成为一类有前途的抗癌剂[5]。一些天然和合成的化合物已被报告为HDACIS。几乎所有HDACIS都包括三个部分：金属结合，接头和表面识别结构域[6]。

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《Chinese international peptide symposium》|2011年||共5页
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Dawei Huang; Xiaohui Li; Zhilong Xiu; Norikazu Nishino;
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1. A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)- disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: Design, synthesis and molecular modeling study [J] . HuangD., LiX., WeiY., European Journal of Medicinal Chemistry: Chimie Therapeutique . 2012,第Null期

机译：作为组蛋白脱乙酰基酶抑制剂的一系列新的l-2-苄氧基羰基氨基-8-（2-吡啶基）-二硫基辛酸衍生物：设计，合成和分子模型研究
2. Aryl butenoic acid derivatives as a new class of histone deacetylase inhibitors: synthesis, in vitro evaluation, and molecular docking studies [J] . Peruze AYHAN ESJYOK, Ozlem SEVEN, Guluzar EYMUR Turkish journal of chemistry . 2014,第2期

机译：芳基丁烯酸衍生物作为一类新的组蛋白脱乙酰基酶抑制剂：合成，体外评估和分子对接研究
3. Aryl butenoic acid derivatives as a new class of histone deacetylase inhibitors: synthesis, in vitro evaluation, and molecular docking studies [J] . PERUZE AYHAN E??YOK, ?ZLEM SEVEN, GüLüZAR EYMUR, Turkish journal of chemistry . 2014,第2期

机译：芳基丁烯酸衍生物作为一类新的组蛋白脱乙酰基酶抑制剂：合成，体外评估和分子对接研究
4. Synthesis, Evaluation and Molecular Modeling Study of L-2-amino-7/8-Bromoalkanoic Acid Derivatives as Histone Deacetylase Inhibitors [C] . Dawei Huang, Xiaohui Li, Zhilong Xiu, Chinese international peptide symposium . 2011

机译：L-2-氨基-7 / 8-溴烷酸衍生物作为组蛋白脱乙酰酶抑制剂的合成，评价和分子建模研究
5. I. Structure-based molecular modeling and synthesis of indole derivatives as non-phenolic analogues of mycophenolic acid. II. 3D-QSAR studies using CoMFA on homotropane and tropane derivatives as dopamine transporter and serotonin transporter ligands. [D] . El-Araby, Moustafa El-Sayed. 2001

机译：I.基于结构的分子模型和吲哚衍生物作为霉酚酸的非酚类似物的合成。二。 3D-QSAR研究使用CoMFA对高碘烷和托烷衍生物作为多巴胺转运蛋白和5-羟色胺转运蛋白配体的研究。
6. Design Synthesis Molecular Modeling and Biological Evaluation of Novel Amine-based Histone Deacetylase Inhibitors [O] . Dr. Hazem Abdelkarim, Dr. Raghupathi Neelarapu, Antonett Madriaga, -1

机译：新型基于胺的组蛋白脱乙酰基酶抑制剂的设计合成分子建模和生物学评估
7. Aryl butenoic acid derivatives as a new class of histone deacetylase inhibitors: synthesis, in vitro evaluation, and molecular docking studies [O] . Esiyok Ayhan Peruze, Seven Ozlem, Eymur Guluzar, 2014

机译：芳基丁烯酸衍生物作为新型组蛋白脱乙酰基酶抑制剂：合成，体外评估和分子对接研究

Synthesis, Evaluation and Molecular Modeling Study of L-2-amino-7/8-Bromoalkanoic Acid Derivatives as Histone Deacetylase Inhibitors

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