许凤荣

作品数:14被引量:8H指数:2
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供职机构:北京大学更多>>
发文主题:化合物分泌酶Β-分泌酶类化合物MEK更多>>
发文领域:医药卫生化学工程理学更多>>
发文期刊:《中国药物化学杂志》《Journal of Chinese Pharmaceutical Sciences》《中国医药工业杂志》《中国科技论文》更多>>
所获基金:国家自然科学基金国家教育部博士点基金国家重点基础研究发展计划北京市自然科学基金更多>>
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3H-吡喃并[2,3-d]嘧啶-4,7-二酮类MEK激酶抑制剂的设计、合成及初步活性评价
《中国科技论文》2015年第24期2823-2829,共7页孙静 牛彦 许凤荣 梁磊 王超 徐萍 
国家自然科学基金资助项目(21172012);高等学校博士学科点专项科研基金资助项目(20120001110010)
Ras/Raf/MEK/ERK通路在许多人类肿瘤中均为异常活化,通过抑制MEK激酶阻断此信号通路成为小分子抗癌药物开发的良好靶标。将前期研究工作发现的嘧啶-4(3H)-酮骨架结构与香豆素骨架进行拼合,设计了3H-吡喃并[2,3-d]嘧啶-4,7-二酮骨架,并...
关键词:药物化学 MEK抑制剂 抗肿瘤 3H-吡喃并[2 3-d]嘧啶-4 7-二酮 
Design, synthesis and biological evaluation of sulfonamide flavone derivatives as potential 20S proteasome inhibitors
《Journal of Chinese Pharmaceutical Sciences》2014年第9期626-630,共5页杨冠宇 孙琦 王超 梁磊 许凤荣 牛彦 徐萍 
The National Natural Science Foundation of China(Grant No.21202003);the National Basic Research Program of China(Grant No.2012CB518000);the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010)
A new series of sulfonamide flavone derivatives are designed as non-covalent inhibitors of proteasome assisted with computer-aided drug design (CADD). The desired compounds were synthesized successfully and the biol...
关键词:Sulfonamide flavone derivatives Non-covalent inhibitor CADD 20S proteasome inhibitor SELECTIVITY 
Synthetic strategies for piperazine derivatives
《Journal of Chinese Pharmaceutical Sciences》2014年第8期572-577,共6页翟亚亚 闫钢 黄文杰 牛彦 许凤荣 梁磊 王超 徐萍 
National Basic Research Program of China(Grant No.2012CB518000);the National Natural Science Foundation of China(Grant No.21172012);the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010)
As important constitutes in many drugs, piperazine comprised compounds are of great interest for drug design. In this paper, two piperazine-based compounds were synthesized for the first time, with different strategie...
关键词:PIPERAZINE Synthesis strategy ISOTHIOCYANATE Michael addition Friedel-Crafts acylation 
Design and synthesis of benzimidamides as potential BACE1 inhibitors
《Journal of Chinese Pharmaceutical Sciences》2012年第2期124-131,共8页高海飞 牛彦 许凤荣 梁磊 周博 李勇剑 王超 刘鹏 徐萍 
National Natural Science Foundation of China(Grant No. 21002002);Specialized Research Fund for the Doctoral Program of Higher Education of China (Grant No. 200800011057)
Computer aided fragment-based lead discovery has been successfully applied to the design of inhibitors of aspartyl protease enzyme β-secretase(BACE1).A benzimidamide fragment,which binds to the two catalytic aspart...
关键词:Alzheimer's disease BACE1 inhibitors CADD Benzimidamide 
Design,synthesis and biological evaluation of pyrrolidinone analogs as potential 20S proteasome inhibitors
《Journal of Chinese Pharmaceutical Sciences》2011年第6期564-571,共8页李勇剑 许凤荣 牛彦 邹晓民 袁悦 高海飞 王超 杨冠宇 孙琦 徐萍 
Beijing Natural Science Foundation(Grant No. 7112088)
A novel series of pyrrolidinone analogs that are designed as Michael addition acceptors to react irreversibly with the proteasome active site Thr1O~γhave been synthesized.Although biological evaluation results show t...
关键词:PYRROLIDINONE 20S proteasome Peptidomimetic backbone 
Synthesis of acyclic analogs of Syringolin A as potential 20S proteasome inhibitors
《Journal of Chinese Pharmaceutical Sciences》2010年第6期423-435,共13页袁悦 邹晓民 牛彦 许凤荣 牟科 周博 王超 李勇剑 杨冠宇 徐萍 
National Natural Science Foundation of China (Grant No.20772008 and 30772650)
A series of acyclic analogs of natural product Syringolin A (SylA) were designed and synthesized during our synthetic efforts for SylA. These acyclic analogs were prepared through a seven-step linear strategy, with ...
关键词:Syringolin A 20S proteasome Peptidyl vinyl amide 
Structure-based design of hexahydropyrimidin-5-ols as novel non-peptidic β-secretase inhibitors
《Journal of Chinese Pharmaceutical Sciences》2010年第5期341-345,共5页周博 牛彦 邹晓民 许凤荣 袁悦 王超 高海飞 刘鹏 徐萍 
National Natural Science Foundation of China (Grant No.20772008 and 30772650)
Based upon the crystal structure of a previously reported fragment hit that binds to Corresponding author. β-secretase, a novel series of non-peptidic small-molecule β-secretase inhibitors, namely hexahydropyrimidin...
关键词:β-Secretase inhibitors Hexahydropyrimidin-5-ols Structure-based drug design Computer-aided drug design 
全新结构钾离子通道开放剂先导化合物的设计合成与QSAR的研究被引量:1
《中国药物化学杂志》2001年第4期198-204,共7页王炜 崔智勇 许凤荣 李仁利 杨明娜 李长龄 苏阳 周家驹 
国家自然科学基金资助课题 (3 9670 85 4 )
在进一步研究钾离子开放剂的药效团基础上设计并合成了 1 7个化合物 ,连同以前合成的4个化合物用SYBYL软件优化了它们的构象并计算了芳环中心与氢键接受原子间的距离 (Ar HA)、芳环中心与疏水性部分中心的距离 (Ar Hy)、氢键接受原子与...
关键词:钾离子开放剂 药效团 定量构效关系 设计合成 
钙调素拮抗剂亲脂区与亲水区之间连接链距离的研究
《北京医科大学学报》1997年第5期433-437,共5页雷小平 张亮仁 许凤荣 
国家自然科学基金!3930812
目的:研究钙调素拮抗剂亲脂区与亲水区之间连接链最佳的距离。方法:采用Fibonacci寻找法设计并合成了不同长度侧链的1,2-二苯乙烯类钙调素拮抗剂。结果:它们的拮抗活性表明,随着连接亲水部分氨基与亲脂苦环部分的碳链的增长,其...
关键词:钙调蛋白 拮抗剂 亲脂区 分子图形学 中间连接链 
胍基取代的1,2-二苯乙烯类钙调素拮抗剂的合成被引量:1
《中国医药工业杂志》1997年第6期251-253,共3页雷小平 许凤荣 刘波 
国家自然科学基金
合成了三个胍基取代的1,2-二苯乙烯类钙调素拮抗剂。引入胍基可使拮抗剂活性提高,强于三氟拉嗪。
关键词:钙调素拮抗剂 胍基 二苯基己烯-1 SN2反应 合成 
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