检索结果-南通市图书馆

Treatment of severe radiation proctitis with high dosage of vitamin C in combination with cyclooxygenase-2 inhibitor

引用

Radiation Medicine and Protection 2024年第2期5卷 113-117页

作者： Han Wu Miaomiao Liu Huangang Jiang Hui Xu Jin Peng Jing Dai Fuxiang Zhou Department of Radiation and Medical Oncology Zhongnan HospitalWuhan UniversityWuhan 430007China Hubei Key Laboratory of Tumor Biological Behaviors Zhongnan HospitalWuhan UniversityWuhan 430007China Hubei Clinical Cancer Study Center Zhongnan Hospital of Wuhan UniversityWuhan 430007China

Objective:To explore the new treatment strategies for radiation proctitis,which is the most common complication of pelvic tumor ***:Four cases of patients with severe radiation proctitis were treated with high-dosage vitamin C(VC,12–24 g/d,iv)combined with cyclooxygenase-2(cyclooxygenase-2,COX-2)***:For these four cases,the diarrhea,hematochezia,tenesmus,pain,and other symptoms were significantly *** edema of the rectal wall is also significantly improved in the imaging ***:The high-dosage VC combined with the treatment of severe radiation proctitis is safe and effective.

关键词： Radiation proctitis Vitamin C cyclooxygenase-2 inhibitor Radiotherapy

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Design,synthesis and pharmacological evaluation of 4-[2-alkylthio-5(4)-(4-substitutedphenyl)imidazole-4(5)yl]benzenesulfonamides as selective COX-2 inhibitors

引用

Acta Pharmacologica Sinica 2007年第8期28卷 1254-1260页

作者： Mona SALIMI Mohammad Hossein GHAHREMANI Nima NADERI Mohsen AMINI Elika SALIMI Massoud AMANLOU Khosrou ABDI Raha SALEHI Abbas SHAFIEE Research and Development Center Pasteur Institute of IranKasasIran Department of Pharmacology and Toxicology Faculty of Pharmacy and Pharmaceutical Sciences Research CenterTehran University of Medical SciencesTehranIran Neuroscience Research Center Shahid Beheshti University of Medical SciencesTehranIran Department of Medicinal Chemistry Faculty of Pharmacy and Pharmaceutical Sciences Research CenterTehran University of Medical SciencesTehranIran Department of Pharmacology Faculty of PharmacyMazanderan University of Medical SciencesSariIran

Aim:To design and synthesize a series of benzenesulfonamide derivatives,4-[2-alkylthio-5（4）-（4-substitutedphenyl）imidazole-4（5）-yl]benzenesulfonamides（4a-4j）,which are intended to act as cyclooxygenase-2（COX-2）inhibitors with goodCOX-2 inhibitor activity,and which will exert anti-inflammatory activities in ***:Benzenesulfonamide derivatives were designed and synthesized throughmulti-step chemical *** the synthesized compounds were evaluated inan in vitro *** active compound 4a-af was selected for further evaluationin a carrageenan-induced rat paw edema ***:Docking studies showedthat compound 4 bind into the primary binding site of COX-2 with the sulfonamideSO2NH2moiety interacting with the secondary pocket amino acid *** thein vitro assay,compound 4 inhibited COX-2 with an inhibition concentration IC50value of 1.23-8 nmol/L,compared to celecoxib with IC50 value of 1.5 nmol/***-pound 4b and 4c had good potency and selectivity in comparison to the *** the in vivo model,compound 4a-4f exhibited a moderate potency to inhibit 50%carrageenan-induced paw edema with value of 1.58-4.3 mg/*** the latterexperiment,compound 4c was the most active ***:The anti-inflammatory effects obtained for compound 4a-4j could be due to the presenceof fluorine or hydrogen substituents in the para position of the phenyl ring ofthese compounds.

关键词： cyclooxygenase-2 inhibitor imidazole alkylthio celecoxib

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

环氧合酶-2(COX-2)抑制剂的活性预测与结构聚类研究（英文）

环氧合酶-2(COX-2)抑制剂的活性预测与结构聚类研究（英文）

引用

2019中国化学会第十五届全国计算（机）化学学术会议

作者：秦子健 Yao Xi Shengde Zhang Guiping Tu Aixia Yan 北京化工大学 Department of Pharmaceutical Engineering Beijing University of Chemical Technology

cyclooxygenase-2(COX-2) is an inducible form of the COX enzyme, and is an important target of Nonsteroidal Anti-Inflammatory Drugs(NSAIDs). This work reports the classification study conducted on the biggest COX-2 inhibitor data set so far. Using 2925 diverse COX-2 inhibitors collected from 168 pieces of literature, we applied machine learning methods, support vector machine(SVM) and random forest(RF), to develop 12 classification models. The best SVM and RF models resulted in Matthews correlation coefficient(MCC) values of 0.73 and 0.72 on the validation set, respectively. The 2925 COX-2 inhibitors were reduced to a data set of 1630 molecules by removing intermediately active inhibitors, and 12 new classification models were constructed, yielding MCC values above 0.72 on the validation set. The best MCC value of the external test set was predicted to be 0.68 by the RF model using ECFP fingerprints. Moreover, we clustered the 2925 COX-2 inhibitors into eight subsets based on their MACCS fingerprints by t-distributed stochastic neighbor embedding(t-SNE) and k-means and investigated the structural features of each subset. We also analyzed the diversity of these COX-2 inhibitors and three types of descriptors(MACCS fingerprints, ECFP fingerprints, and CORINA descriptors). Finally, some useful suggestions on highly/weakly active COX-2 inhibitors were put forward. We identified substructures important for activity including halogen, carboxyl, sulfonamide, and methanesulfonyl groups, as well as the aromatic nitrogen atoms. We hope the models developed in this study could serve as useful tools for compound screening prior to lab tests.

关键词： cyclooxygenase-2 inhibitor support vector machine random forest structures clustering

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：