Structure-activity relationships of indole compounds derived from combretastatin A4: synthesis and biological screening of 5-phenylpyrrolo(3,4-a)carbazole-1,3-diones as potential antivascular agents.

Ty N; Dupeyre G; Chabot GG; Seguin J; Quentin L; Chiaroni A; Tillequin F; Scherman D; Michel S; Cachet X

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Structure-activity relationships of indole compounds derived from combretastatin A4: synthesis and biological screening of 5-phenylpyrrolo(3,4-a)carbazole-1,3-diones as potential antivascular agents.

【24h】

Structure-activity relationships of indole compounds derived from combretastatin A4: synthesis and biological screening of 5-phenylpyrrolo(3,4-a)carbazole-1,3-diones as potential antivascular agents.

机译：康布雷他汀A4衍生的吲哚化合物的结构活性关系：5-苯基吡咯并（3,4-a）咔唑-1,3-二酮作为潜在的抗血管药物的合成和生物学筛选。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A series of 5-(3',4',5'-trimethoxyphenyl)pyrrolo[3,4-a]carbazole-1,3(2H,10H)-diones was designed as cis-restricted analogues of 3-aroylindoles, arylthioindoles and 3-benzylidoneindolin-2-ones derived from combretastatin A4 (CA-4). Starting from various indoles, compounds were synthesized by means of a convenient two-step procedure involving a one-pot multicomponent reaction as key step. Intermediate tetrahydro[3,4-a]carbazoles and their corresponding carbazoles were submitted to biological screening tests involved in antivascular action, including the cytotoxicity against murine B16 melanoma cells, the rounding up of endothelial cells (EA.hy 926) and the inhibition of tubulin polymerization. Of the 31 compounds screened, those bearing a methoxy group at the 8-position endowed significant biological activities. A carbazole compound 30 was identified as a promising candidate for further development of novel vascular targeting agents.

机译：一系列5-（3'，4'，5'-三甲氧基苯基）吡咯并[3,4-a]咔唑-1,3（2H，10H）-二酮被设计为3-芳基吲哚，芳基硫代吲哚的顺式限制类似物衍生自康维他汀A4（CA-4）的3-苄基二氢吲哚-2-酮。由各种吲哚开始，化合物通过方便的两步法合成，其中一锅多组分反应为关键步骤。中间体四氢[3,4-a]咔唑及其相应的咔唑已进行了涉及抗血管作用的生物学筛选试验，包括对鼠B16黑色素瘤细胞的细胞毒性，内皮细胞的聚集（EA.hy 926）和对H16的抑制作用。微管蛋白聚合。在筛选的31种化合物中，在8位带有甲氧基的化合物具有明显的生物活性。咔唑化合物30被确定为新型血管靶向剂的进一步开发的有希望的候选者。

著录项

来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共14页
作者
Ty N; Dupeyre G; Chabot GG; Seguin J; Quentin L; Chiaroni A; Tillequin F; Scherman D; Michel S; Cachet X;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词

相似文献

外文文献
中文文献

1. Structure-activity relationships of indole compounds derived from combretastatin A4: synthesis and biological screening of 5-phenylpyrrolo(3,4-a)carbazole-1,3-diones as potential antivascular agents. [J] . Ty N, Dupeyre G, Chabot GG, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

机译：康布雷他汀A4衍生的吲哚化合物的结构活性关系：5-苯基吡咯并（3,4-a）咔唑-1,3-二酮作为潜在的抗血管药物的合成和生物学筛选。
2. Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents. [J] . Ty N, Dupeyre G, Chabot GG, Bioorganic and medicinal chemistry . 2008,第15期

机译：作为潜在的抗血管药物的6-甲氧基-3-（3'，4'，5'-三甲氧基苯甲酰基）-1H-吲哚（BPR0L075）的新双取代类似物的合成和生物学评估。
3. Synthesis and Structure-Activity Relationships of Constrained Heterocyclic Analogues of Combretastatin A4 [J] . Martin Arthuis, Renee Pontikis, Guy G. Chabot ChemMedChem . 2011,第9期

机译：Combretastatin A4受限杂环类似物的合成及其构效关系
4. Biological activities and structure-activity relationship of substitution compounds of N-2-(3-mdolyl)ethylsucdnamic acid and N-2-(l-naphthyl)ethylsuccinamic acid, derived from a new category of root-promoting substances, N-(phenethyl)succinamic ac [C] . Mihoko Itagaki, Hiroshi Soejima, Ko Ishii, Symposium of the International Society of Root Research . 2003

机译：N-2-（3-乳丙基）乙基 Sucdnumic酸和N-2-（L-萘基）乙基琥珀酸的生物活性和结构 - 活性关系，衍生自新类促进物质，N-（苯乙基）琥珀酰胺AC
5. Synthesis and Biological Evaluation of Novel Resveratrol and Combretastatin A4 Derivatives as Potent Anti-Cancer Agents. [D] . Madadi, Nikhil Reddy. 2014

机译：新型白藜芦醇和Combretastatin A4衍生物作为强效抗癌药的合成及生物学评价。
6. Novel Pyrazolo34-dpyrimidine Derivatives as Potential Antitumor Agents: Exploratory Synthesis Preliminary Structure-Activity Relationships and in Vitro Biological Evaluation [O] . Hai-Yun He, Jin-Ni Zhao, Ruo Jia, 2011

机译：新型吡唑并34-d嘧啶衍生物作为潜在的抗肿瘤药：探索性合成初步的结构活性关系和体外生物学评价
7. Pyridonecarboxylic Acids as Antibacterial Agents Part XVII. 5-Alkoxyimidazoquinolones as Potential Antibacterial Agents. Synthesis and Structure-Activity Relationships. [O] . Masahiro FUJITA, Hiroshi EGAWA, Teruyuki MIYAMOTO, 1996

机译：吡啶羧酸作为抗菌剂部分XVII。 5-烷氧基咪唑喹酮作为潜在的抗菌剂。合成与结构活动关系。

Structure-activity relationships of indole compounds derived from combretastatin A4: synthesis and biological screening of 5-phenylpyrrolo(3,4-a)carbazole-1,3-diones as potential antivascular agents.

摘要

著录项

相似文献

相关主题

期刊订阅