北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学药学院  > 期刊论文
学科主题: 药学
题名:
Synthesis and Bioactivity of N-Benzoyl-N ′-[5-(2 ′-substituted phenyl)-2-furoyl] Semicarbazide Derivatives
作者: Cui, Zining1; Ling, Yun1; Li, Baoju2; Li, Yongqiang1; Rui, Changhui1; Cui, Jingrong3; Shi, Yanxia2; Yang, Xinling1
关键词: chitin synthesis inhibitors ; benzoylphenylurea ; semicarbazide ; synthesis ; bioactivity
刊名: MOLECULES
发表日期: 2010-06-01
DOI: 10.3390/molecules15064267
卷: 15, 期:6, 页:4267-4282
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Organic
研究领域[WOS]: Chemistry
关键词[WOS]: QUANTITATIVE STRUCTURE-ACTIVITY ; INSECT GROWTH-REGULATORS ; BENZOYLPHENYLUREAS ; SUBSTITUENTS ; DESIGN
英文摘要:

In order to find novel chitin synthesis inhibitors (CSIs) with good activity, benzoylphenylurea, a typical kind of CSIs, was chosen as the lead compound and 15 novel derivatives containing furan moieties were designed by converting the urea linkage of benzoylphenylureas into a semicarbazide and changing the aniline part into furoyl groups. The title compounds were synthesized by the reaction of substituted benzoyl isocyanates with 5-(substituted phenyl)-2-furoyl hydrazine, and the structures were confirmed by IR, (1)H-NMR, elemental analysis and single crystal X-ray diffraction analyses (compound E2). The bioassay results indicated that the title compounds exhibit good insecticidal activity, especially towards Plutella xylostella L., but had lower fungicidal activity. Inspiringly, the title compounds possessed obvious anticancer activity against human promyelocytic leukemic cell line (HL-60), and some of the title compounds also had activity against human hepatocellular carcinoma cell line (Bel-7402), human gastric carcinoma cell line (BGC-823), and human nasopharyngeal carcinoma cell line (KB). The results indicated that the linkage in the lead compounds was important to the bioactivity and spectra. The modification on the urea linkage is an effective strategy to discover new pesticide and drug candidates.

语种: 英语
所属项目编号: 2006AA10A201 ; 2010CB126104 ; 20972185
项目资助者: National High Technology Research and Development Program of China ; National Key Project for Basic Research ; National Natural Science Foundation of China ; Scientific Research Foundation of the Graduate School of China Agricultural University
WOS记录号: WOS:000279207300032
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/52989
Appears in Collections:北京大学药学院_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.China Agr Univ, Dept Appl Chem, Coll Sci, Key Lab Pesticide Chem & Applicat,Minist Agr, Beijing 100193, Peoples R China
2.Chinese Acad Agr Sci, Inst Vegetables & Flowers, Beijing 100081, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Cui, Zining,Ling, Yun,Li, Baoju,et al. Synthesis and Bioactivity of N-Benzoyl-N ′-[5-(2 ′-substituted phenyl)-2-furoyl] Semicarbazide Derivatives[J]. MOLECULES,2010,15(6):4267-4282.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Cui, Zining]'s Articles
[Ling, Yun]'s Articles
[Li, Baoju]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Cui, Zining]‘s Articles
[Ling, Yun]‘s Articles
[Li, Baoju]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace