国家自然科学基金(21172014)

作品数:13被引量:7H指数:1
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相关作者:刘俊义张志丽王孝伟王锰田超更多>>
相关机构:北京大学更多>>
相关期刊:《中国药物化学杂志》《北京大学学报(医学版)》《药学学报》《Chemical Research in Chinese Universities》更多>>
相关主题:DERIVATIVES叶酸拮抗剂ACTIVITIES蛋氨酸合成酶抗肿瘤更多>>
相关领域:医药卫生生物学理学化学工程更多>>
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新型嘧啶单环类非经典叶酸拮抗剂的合成及抗肿瘤活性研究
《有机化学》2021年第2期776-787,共12页丛婧 方芳 薛良敏 王锰 田超 王孝伟 刘俊义 张志丽 
国家自然科学基金(No.21172014)资助项目.
以课题组前期设计合成的非经典叶酸拮抗剂6-(4'-甲基苯乙基)-N5-氯乙酰基-2,4-二氨基哌啶并[3,2-d]嘧啶(wm-8.2)为先导化合物,将wm-8.2中的哌啶并嘧啶双环结构简化为嘧啶单环结构,以提高分子柔韧性并简化分子结构,根据6-位空间占位设计...
关键词:非经典叶酸拮抗剂 新型嘧啶单环类衍生物 抗肿瘤活性 二氢叶酸还原酶抑制活性 分子对接 
Pyridin-2(1H)-ones as HIV-1 NNRTIs:a combinatorial optimization strategy
《Journal of Chinese Pharmaceutical Sciences》2020年第2期79-89,共11页Xixi Li Qian Liu Tao Sheng Junyi Liu Xiaowei Wang 
National Natural Science Foundation of China(Grant No.21172014,20972011 and 21042009).
With rapid spread of HIV(human immunodeficiency virus) on a global scale and increasingly severe drug-resistance of it,it is urgently necessary to develop novel effective anti-HIV drugs.Non-nucleoside reverse transcri...
关键词:HIV-1 Reverse transcriptase DRUG-RESISTANCE NNRTIS Pyridinone derivatives 
Similar pyridinone compounds with different activities of anti-HIV-1 reverse transcriptase被引量:1
《Journal of Chinese Pharmaceutical Sciences》2018年第7期469-477,共9页Yunqi Liu Xixi Li Xiaodong Dou Chao Tian Zhili Zhang Junyi Liu Xiaowei Wang 
The National Natural Science Foundation of China(Grant No.21172014,20972011 and 21042009)
Among the structurally diverse NNRTIs, pyridinone scaffolds demonstrate high potency against HIV-1 wild type and drug-resistant strains. During the optimization of our pyridinone compound 1(LAM-trans), we found that...
关键词:Pyridinone derivatives HIV-1 Reverse transcriptase Halogen bond Molecular docking study 
基于4-氨基-5-甲酰基-8,10-二去氮杂四氢叶酸二乙酯侧链的水解反应条件优化
《北京大学学报(医学版)》2017年第4期714-718,共5页袁蒙蒙 王锰 刘俊义 张志丽 
国家自然科学基金(21172014)资助~~
目的:改进经典抗叶酸类药物关键中间体4-氨基-5-甲酰基-8,10-二去氮杂四氢叶酸二乙酯侧链的水解条件。方法:以经典叶酸拮抗剂侧链N-(4-氨基苯甲酰)-L-谷氨酸二乙酯(1)为反应原料,尝试了氢氧化钠(Na OH)和氢氧化钾(KOH)2种碱催化、20~180...
关键词:叶酸拮抗剂 叶酸二乙酯类似物 水解反应 
Docking and field-based QSAR studies of S-DABOs as HIV-1 reverse transcriptase inhibitors被引量:1
《Journal of Chinese Pharmaceutical Sciences》2017年第7期512-520,共9页樊宁宁 刘振明 王孝伟 刘俊义 
National Natural Science Foundation of China(Grant No.21172014,20972011,21042009,21272017 and 81172917);Grants from the Ministry of Science and Technology of China(Grant No.2009ZX09301-010)
HIV-1 reverse transcriptase(RT) inhibitors are major components of HAART(highly active antiviral therapy). The S-DABOs(dihydro-alkylthio-benzyl-oxopyrimidines) series and their similar skeletons have exhibited p...
关键词:HIV-1 reverse transcriptase S-DABOs Molecular docking Field-based QSAR 
蛋氨酸合成酶抑制剂的研究进展被引量:1
《中国药物化学杂志》2017年第6期466-476,共11页王锰 仰佳佳 薛良敏 李灏 刘俊义 张志丽 
国家自然科学基金项目(21172014);国家自然科学青年基金项目(21302007)
在过去的70年里,叶酸拮抗剂对恶性肿瘤、微生物和寄生虫的感染、慢性炎症等疾病的治疗起到了举足轻重的作用。具有更好性质和活性的新型叶酸拮抗剂的发现仍然吸引着学术界和工业界的广泛关注。蛋氨酸合成酶作为叶酸代谢的关键酶,其对维...
关键词:蛋氨酸合成酶 钴胺素 蛋氨酸合成酶抑制剂 抗肿瘤 
Design, synthesis and activity evaluation of novel pyridinone derivatives as anti-HIV-1 dual(RT/IN) inhibitors被引量:1
《Journal of Chinese Pharmaceutical Sciences》2017年第1期31-44,共14页Quanzhi Yang Tao Sheng Ningning Fan Yameng Hao Yuanyuan Cao Ying Guo Zhili Zhang Chao Tian Junyi Liu Xiaowei Wang 
National Natural Science Foundation of China(Grant No.21172014,812111023 and 81172733);grants from the Ministry of Science and Technology of China(Grant No.200 9ZX09301-010)
Three series of novel anti-immunodeficiency virus 1 (HIV-1) dual (RT/1N) inhibitors were rationally designed by introducing a functioning diketo acid (DKA) into pyridin-2-one scaffold. To efficiently analyze inh...
关键词:Pyridinone derivatives HIV-1 dual inhibitor Reverse transcriptase INTEGRASE 
Design, Synthesis and Activities of Aziridine Derivatives of N^5-Methyltetrahydrofolate Against Methionine Synthase被引量:2
《Chemical Research in Chinese Universities》2015年第5期742-745,共4页DENG Xiling GUO Ying TIAN Chao LIU Junyi WANG Xiaowei ZHANG Zhili 
Supported by the National Natural Science Foundation of China(No.21172014).
Aziridine derivatives of N^5-methyltetrahydrofolate were designed and synthesized based on the mechanism of methionine synthase, and their biological activities were investigated as well. The aziridine derivatives 1 a...
关键词:AZIRIDINE Methionine synthase Ring closure reaction N^5-Methyltetrahydrofolate 
N^5-甲基四氢叶酸类似物的合成及其蛋氨酸合成酶抑制活性研究被引量:1
《中国药物化学杂志》2015年第6期415-423,共9页杜义青 袁蒙蒙 王锰 刘俊义 张志丽 
国家自然科学基金项目(21172014)
目的在蛋氨酸合成酶抑制剂先导化合物的基础上设计合成4-氨基-8,10-二去氮杂-N^5-取代四氢叶酸类似物和4-氨基-8-去氮杂-N^5,N10-二取代四氢叶酸类似物,并对其蛋氨酸合成酶(MS)抑制活性进行评价,以考察N^5位和N10位酰基取代基对活性的影...
关键词:蛋氨酸合成酶 四氢叶酸类似物 抑制剂 抗肿瘤 
Route improvement of 3-substituted-4-(2-methylcyclohexyloxy)-6-phenethylpyridinone
《Journal of Chinese Pharmaceutical Sciences》2014年第4期220-224,共5页刘香宜 曹源源 张羽 杨全志 王孝伟 刘俊义 
National Natural Science Foundation of China(Grant No.20972011,21042009,21172014);grants from the Ministry of Science and Technology of China(Grant No.2009ZX09301010)
trans-3-Isopropyl-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-one, as reverse transcriptase (NNRTIs), exhibited significant potent activity not only against wild-type HIV-1 strains but also on mutant stra...
关键词:HIV-1 Non-nucleoside reverse transcriptase inhibitors Route improvement 
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