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 biological activities of 2-oxocycloalkylsulfonamides
作者: Li, Xinghai1; Yang, Xinling1; Liang, Xiaomei1; Kai, Zhenpeng1; Yuan, Huizu2; Yuan, Dekai1; Zhang, Jianjun1; Wang, Ruiqing3; Ran, Fuxiang3; Qi, Shuhua2; Ling, Yun1; Chen, Fuheng1; Wang, Daoquan1
关键词: 2-oxocycloalkylsulfonamide ; fungicidal activity ; antitumor activity ; QSAR
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2008-04-15
DOI: 10.1016/j.bmc.2008.02.048
卷: 16, 期:8, 页:4538-4544
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
英文摘要:

A series of novel 2-oxocycloalkylsulfonamides ( 4) were synthesized and their structures confirmed by IR, H-1 NMR, and elemental analysis. The bioassay showed that they have fair to excellent fungicidal activities against Botrytis cinerea Pers and Sclerotinia sclerotiorum. Among them, compounds 4A(10), 4A(11), 4A(12), 4B(2), and 4B(3), the EC50 values of which were 2.12, 3.66, 3.96, 2.38, and 2.43 mu g/mL, respectively, displayed excellent fungicidal activity against B. cinerea Pers, and are comparable with commercial fungicide procymidone ( the EC50 value is 2.45 mu g/mL). 3D QSAR against B. cinerea Pers was studied, a statistically significant and chemically meaningful CoMFA model was developed and some compounds which have a high predicted activity were forecasted. In addition, the bioassay also showed that the compounds have good inhibitory activities against human tumor cells HL-60, BGC-823, Bel-7402 and KB. It is interesting to point out that the antitumor activities of compounds 4 are in accordance with their fungicidal activity to a great extent: compounds having relatively best antitumor activities ( 4A10, 4A11, 4A12, and 4B3) also displayed excellent fungicidal activity. (c) 2008 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000255246100033
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53345
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, Key Lab Pesticide Chem & Applicat Technol, Beijing 100094, Peoples R China
2.Chinese Acad Agr Sci, Inst Plant Protect, Beijing 100094, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Li, Xinghai,Yang, Xinling,Liang, Xiaomei,et al. Synthesis and biological activities of 2-oxocycloalkylsulfonamides[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(8):4538-4544.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Li, Xinghai]'s Articles
[Yang, Xinling]'s Articles
[Liang, Xiaomei]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Li, Xinghai]‘s Articles
[Yang, Xinling]‘s Articles
[Liang, Xiaomei]‘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
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

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